Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 32, Issue 1 (2017)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 32, Issue 1 (2017)

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Research Article

Article
The effects of nifedipine on respiratory mechanics investigated by theend-inflation occlusion method in the rat
Alessandro Rubini, Vincenzo Catena, Daniele del Monte & Gerardo Bosco
Pages: 1-4
Published online: 21 Oct 2016
AbstractforThe effects of nifedipine on respiratory mechanics investigated by theend-inflation occlusion method in the rat | Full Text | References | PDF (414.1 KB)
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Review Article

Review
Insights into the role of reactive sulfhydryl groups of Carbonic Anhydrase III and VII during oxidative damage
Daria M. Monti, Giuseppina De Simone, Emma Langella, Claudiu T. Supuran, Anna Di Fiore & Simona M. Monti
Pages: 5-12
Published online: 21 Oct 2016
AbstractforInsights into the role of reactive sulfhydryl groups of Carbonic Anhydrase III and VII during oxidative damage | Full Text | References | PDF (1.2 MB)
  • 1880 Views
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Open Access

Original Article

Article
Synthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors
Zeynep Soyer, Sirin Uysal, Sulunay Parlar, Ayse Hande Tarikogullari Dogan & Vildan Alptuzun
Pages: 13-19
Published online: 21 Oct 2016
AbstractforSynthesis and molecular docking studies of some 4-phthalimidobenzenesulfonamide derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors | Full Text | References | PDF (755.2 KB)
  • 3505 Views
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Open Access

Research Article

Article
Diethylalkylsulfonamido(4-methoxyphenyl)methyl)phosphonate/phosphonic acid derivatives act as acid phosphatase inhibitors: synthesis accompanied by experimental and molecular modeling assessments
Nahid Alimoradi, Mohammad Reza Ashrafi-Kooshk, Mohsen Shahlaei, Shabnam Maghsoudi, Hadi Adibi, Ross P. McGeary & Reza Khodarahmi
Pages: 20-28
Published online: 21 Oct 2016
AbstractforDiethylalkylsulfonamido(4-methoxyphenyl)methyl)phosphonate/phosphonic acid derivatives act as acid phosphatase inhibitors: synthesis accompanied by experimental and molecular modeling assessments | Full Text | References | PDF (1 MB)
  • 1328 Views
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Open Access
Article
Novel FFA1 (GPR40) agonists containing spirocyclic periphery: polar azine periphery as a driver of potency
Mikhail Krasavin, Alexey Lukin, Daria Bagnyukova, Nikolay Zhurilo, Ihor Zahanich & Sergey Zozulya
Pages: 29-36
Published online: 26 Oct 2016
AbstractforNovel FFA1 (GPR40) agonists containing spirocyclic periphery: polar azine periphery as a driver of potency | Full Text | References | PDF (1.5 MB) | Supplemental
  • 1336 Views
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Open Access
Article
A class of carbonic anhydrase I – selective activators
Erol Licsandru, Muhammet Tanc, Istvan Kocsis, Mihail Barboiu & Claudiu T. Supuran
Pages: 37-46
Published online: 01 Nov 2016
AbstractforA class of carbonic anhydrase I – selective activators | Full Text | References | PDF (1.9 MB)
  • 2110 Views
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Open Access
Article
Carbonic anhydrase from Apis mellifera: purification and inhibition by pesticides
Ercan Soydan, Ahmet Güler, Selim Bıyık, Murat Şentürk, Claudiu T. Supuran & Deniz Ekinci
Pages: 47-50
Published online: 16 Jan 2017
AbstractforCarbonic anhydrase from Apis mellifera: purification and inhibition by pesticides | Full Text | References | PDF (576.7 KB)
  • 1721 Views
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Open Access
Article
Open saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms
Melissa D’Ascenzio, Paolo Guglielmi, Simone Carradori, Daniela Secci, Rosalba Florio, Adriano Mollica, Mariangela Ceruso, Atilla Akdemir, Anatoly P. Sobolev & Claudiu T. Supuran
Pages: 51-59
Published online: 26 Oct 2016
AbstractforOpen saccharin-based secondary sulfonamides as potent and selective inhibitors of cancer-related carbonic anhydrase IX and XII isoforms | Full Text | References | PDF (1,021.8 KB) | Supplemental
  • 2257 Views
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Open Access

Original Article

Article
Multicomponent pattern and biological activities of seven Asphodeline taxa: potential sources of natural-functional ingredients for bioactive formulations
Marcello Locatelli, Gokhan Zengin, Ahmet Uysal, Simone Carradori, Elisa De Luca, Giuseppe Bellagamba, Abdurrahman Aktumsek & Irina Lazarova
Pages: 60-67
Published online: 24 Oct 2016
AbstractforMulticomponent pattern and biological activities of seven Asphodeline taxa: potential sources of natural-functional ingredients for bioactive formulations | Full Text | References | PDF (937.3 KB)
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Research Article

Article
Isatin: a privileged scaffold for the design of carbonic anhydrase inhibitors
Claudia Melis, Rita Meleddu, Andrea Angeli, Simona Distinto, Giulia Bianco, Clemente Capasso, Filippo Cottiglia, Rossella Angius, Claudiu T. Supuran & Elias Maccioni
Pages: 68-73
Published online: 24 Oct 2016
AbstractforIsatin: a privileged scaffold for the design of carbonic anhydrase inhibitors | Full Text | References | PDF (868.4 KB)
  • 2099 Views
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Open Access
Article
Carbonic anhydrase inhibitory properties of some uracil derivatives
Emir Alper Türkoğlu, Murat Şentürk, Claudiu T. Supuran & Deniz Ekinci
Pages: 74-77
Published online: 18 Jan 2017
AbstractforCarbonic anhydrase inhibitory properties of some uracil derivatives | Full Text | References | PDF (500.2 KB)
  • 1959 Views
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Open Access
Article
Tyrosinase inhibitory components from Aloe vera and their antiviral activity
Jang Hoon Kim, Ju-Yeon Yoon, Seo Young Yang, Seung-Kook Choi, Sun Jung Kwon, In Sook Cho, Min Hee Jeong, Young Ho Kim & Gug Seoun Choi
Pages: 78-83
Published online: 25 Oct 2016
AbstractforTyrosinase inhibitory components from Aloe vera and their antiviral activity | Full Text | References | PDF (960.9 KB) | Supplemental
  • 3861 Views
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Open Access
Article
Discovery of Klotho peptide antagonists against Wnt3 and Wnt3a target proteins using combination of protein engineering, protein–protein docking, peptide docking and molecular dynamics simulations
Shaher Bano Mirza, Ramin Ekhteiari Salmas, M. Qaiser Fatmi & Serdar Durdagi
Pages: 84-98
Published online: 21 Oct 2016
AbstractforDiscovery of Klotho peptide antagonists against Wnt3 and Wnt3a target proteins using combination of protein engineering, protein–protein docking, peptide docking and molecular dynamics simulations | Full Text | References | PDF (2.1 MB)
  • 2369 Views
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Open Access
Article
Synthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity
Mariusz Mojzych, Paweł Tarasiuk, Katarzyna Kotwica-Mojzych, Muhammad Rafiq, Sung-Yum Seo, Michał Nicewicz & Emilia Fornal
Pages: 99-105
Published online: 25 Oct 2016
AbstractforSynthesis of chiral pyrazolo[4,3-e][1,2,4]triazine sulfonamides with tyrosinase and urease inhibitory activity | Full Text | References | PDF (750.2 KB)
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Open Access
Article
Antimicrobial metal-based thiophene derived compounds
Shakeela Yasmeen, Sajjad Hussain Sumrra, Muhammad Safwan Akram & Zahid H. Chohan
Pages: 106-112
Published online: 21 Oct 2016
AbstractforAntimicrobial metal-based thiophene derived compounds | Full Text | References | PDF (815.5 KB)
  • 1861 Views
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Open Access

Original Article

Article
Synthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases
Emilie Evain-Bana, Lucie Schiavo, Christophe Bour, Don Antoine Lanfranchi, Simone Berardozzi, Francesca Ghirga, Denyse Bagrel, Bruno Botta, Gilles Hanquet & Mattia Mori
Pages: 113-118
Published online: 23 Oct 2016
AbstractforSynthesis, biological evaluation and molecular modeling studies on novel quinonoid inhibitors of CDC25 phosphatases | Full Text | References | PDF (1 MB) | Supplemental
  • 1414 Views
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Open Access
Article
Synthesis of new Schiff bases bearing 1,2,4-triazole, thiazolidine and chloroazetidine moieties and their pharmacological evaluation
Nadia G. Kandile, Mansoura I. Mohamed & Hind M. Ismaeel
Pages: 119-129
Published online: 21 Oct 2016
AbstractforSynthesis of new Schiff bases bearing 1,2,4-triazole, thiazolidine and chloroazetidine moieties and their pharmacological evaluation | Full Text | References | PDF (1.1 MB)
  • 3509 Views
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Open Access
Article
Isatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase
Rita Meleddu, Simona Distinto, Angela Corona, Enzo Tramontano, Giulia Bianco, Claudia Melis, Filippo Cottiglia & Elias Maccioni
Pages: 130-136
Published online: 21 Oct 2016
AbstractforIsatin thiazoline hybrids as dual inhibitors of HIV-1 reverse transcriptase | Full Text | References | PDF (1 MB)
  • 2003 Views
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Open Access
Article
Synthesis and bioactivity of several new hetaryl sulfonamides
Parham Taslimi, Afsun Sujayev, Sevgi Mamedova, Pınar Kalın, İlhami Gulçin, Nastaran Sadeghian, Sukru Beydemir, O. Irfan Kufrevioglu, Saleh H. Alwasel, Vagif Farzaliyev & Sabir Mamedov
Pages: 137-145
Published online: 19 Jan 2017
AbstractforSynthesis and bioactivity of several new hetaryl sulfonamides | Full Text | References | PDF (946.1 KB)
  • 2457 Views
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Research Article

Article
Tertiary amine derivatives of chlorochalcone as acetylcholinesterase (AChE) and buthylcholinesterase (BuChE) inhibitors: the influence of chlorine, alkyl amine side chain and α,β-unsaturated ketone group
Xiao-hui Gao, Chao Zhou, Hao-ran Liu, Lin-bo Liu, Jing-jing Tang & Xin-hua Xia
Pages: 146-152
Published online: 01 Nov 2016
AbstractforTertiary amine derivatives of chlorochalcone as acetylcholinesterase (AChE) and buthylcholinesterase (BuChE) inhibitors: the influence of chlorine, alkyl amine side chain and α,β-unsaturated ketone group | Full Text | References | PDF (1.5 MB) | Supplemental
  • 1686 Views
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Open Access
Article
Functional constituents of wild and cultivated Goji (L. barbarum L.) leaves: phytochemical characterization, biological profile, and computational studies
Andrei Mocan, Gökhan Zengin, Mario Simirgiotis, Michaela Schafberg, Adriano Mollica, Dan C. Vodnar, Gianina Crişan & Sascha Rohn
Pages: 153-168
Published online: 18 Jan 2017
AbstractforFunctional constituents of wild and cultivated Goji (L. barbarum L.) leaves: phytochemical characterization, biological profile, and computational studies | Full Text | References | PDF (1.7 MB)
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Original Article

Article
Designing, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides
Halise Inci Gul, Ebru Mete, Sakip Emre Eren, Hiroshi Sakagami, Cem Yamali & Claudiu T. Supuran
Pages: 169-175
Published online: 23 Oct 2016
AbstractforDesigning, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides | Full Text | References | PDF (724.4 KB)
  • 1530 Views
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Open Access

Research Article

Article
Design, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors
Riham I. Ahmed, Essam Eldin A. Osman, Fadi M. Awadallah & Samir M. El-Moghazy
Pages: 176-188
Published online: 24 Oct 2016
AbstractforDesign, synthesis and molecular docking of novel diarylcyclohexenone and diarylindazole derivatives as tubulin polymerization inhibitors | Full Text | References | PDF (1.4 MB)
  • 1930 Views
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Original Article

Article
Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines
Halise Inci Gul, Ebru Mete, Parham Taslimi, Ilhami Gulcin & Claudiu T. Supuran
Pages: 189-192
Published online: 24 Oct 2016
AbstractforSynthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines | Full Text | References | PDF (645.7 KB)
  • 1766 Views
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Open Access
Article
Novel 1-(2-pyrimidin-2-yl)piperazine derivatives as selective monoamine oxidase (MAO)-A inhibitors
Betül Kaya, Leyla Yurttaş, Begüm Nurpelin Sağlik, Serkan Levent, Yusuf Özkay & Zafer Asim Kaplancikli
Pages: 193-202
Published online: 18 Jan 2017
AbstractforNovel 1-(2-pyrimidin-2-yl)piperazine derivatives as selective monoamine oxidase (MAO)-A inhibitors | Full Text | References | PDF (1.2 MB)
  • 1716 Views
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Short Communication

Rapid Communication
Screening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase
Agustín Zavala, Verónica Kovacec, Gustavo Levín, Albertina Moglioni, María Victoria Miranda, Ernesto García, Laura Bonofiglio & Marta Mollerach
Pages: 203-207
Published online: 23 Jan 2017
AbstractforScreening assay for inhibitors of a recombinant Streptococcus pneumoniae UDP-glucose pyrophosphorylase | Full Text | References | PDF (630.2 KB)
  • 1262 Views
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Research Article

Article
Synthesis, characterization and in vitro inhibition of metal complexes of pyrazole based sulfonamide on human erythrocyte carbonic anhydrase isozymes I and II
Nurgün Büyükkıdan, Bülent Büyükkıdan, Metin Bülbül, Rahmi Kasımoğulları & Samet Mert
Pages: 208-213
Published online: 23 Jan 2017
AbstractforSynthesis, characterization and in vitro inhibition of metal complexes of pyrazole based sulfonamide on human erythrocyte carbonic anhydrase isozymes I and II | Full Text | References | PDF (656.5 KB) | Supplemental
  • 1298 Views
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Open Access
Article
Exhaustive CoMFA and CoMSIA analyses around different chemical entities: a ligand-based study exploring the affinity and selectivity profiles of 5-HT1A ligands
Sara Guariento, Silvia Franchini, Michele Tonelli, Paola Fossa, Claudia Sorbi, Elena Cichero & Livio Brasili
Pages: 214-230
Published online: 23 Jan 2017
AbstractforExhaustive CoMFA and CoMSIA analyses around different chemical entities: a ligand-based study exploring the affinity and selectivity profiles of 5-HT1A ligands | Full Text | References | PDF (2.8 MB) | Supplemental
  • 1074 Views
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Open Access
Article
A novel proton transfer salt of 2-amino-6-sulfamoylbenzothiazole and its metal complexes: the evaluation of their inhibition effects on human cytosolic carbonic anhydrases
Zeynep Alkan Alkaya, Halil İlkimen, Cengiz Yenikaya, Yasemin Kaygısız, Metin Bülbül, Tuncay Tunç & Musa Sarı
Pages: 231-239
Published online: 19 Jan 2017
AbstractforA novel proton transfer salt of 2-amino-6-sulfamoylbenzothiazole and its metal complexes: the evaluation of their inhibition effects on human cytosolic carbonic anhydrases | Full Text | References | PDF (1,019.7 KB) | Supplemental
  • 951 Views
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Open Access
Article
A new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability
Chiara Fulci, Dante Rotili, Anastasia De Luca, Lorenzo Stella, Blasco Morozzo della Rocca, Mariantonietta Forgione, Veronica Di Paolo, Antonello Mai, Mattia Falconi, Luigi Quintieri & Anna M. Caccuri
Pages: 240-247
Published online: 18 Jan 2017
AbstractforA new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability | Full Text | References | PDF (1.4 MB) | Supplemental
  • 1483 Views
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Article
The role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A1 and A2A receptor affinity and selectivity profiles
Lucia Squarcialupi, Marco Betti, Daniela Catarzi, Flavia Varano, Matteo Falsini, Annalisa Ravani, Silvia Pasquini, Fabrizio Vincenzi, Veronica Salmaso, Mattia Sturlese, Katia Varani, Stefano Moro & Vittoria Colotta
Pages: 248-263
Published online: 23 Jan 2017
AbstractforThe role of 5-arylalkylamino- and 5-piperazino- moieties on the 7-aminopyrazolo[4,3-d]pyrimidine core in affecting adenosine A1 and A2A receptor affinity and selectivity profiles | Full Text | References | PDF (2 MB) | Supplemental
  • 1378 Views
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Open Access
Article
Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B
Rita Meleddu, Simona Distinto, Roberto Cirilli, Stefano Alcaro, Matilde Yanez, Maria Luisa Sanna, Angela Corona, Claudia Melis, Giulia Bianco, Peter Matyus, Filippo Cottiglia & Elias Maccioni
Pages: 264-270
Published online: 18 Jan 2017
AbstractforThrough scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B | Full Text | References | PDF (1.2 MB)
  • 1286 Views
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Short Communication

Rapid Communication
Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R
Cornelius Hempel, Frank Totzke, Christoph Schächtele, Abdulkarim Najjar, Wolfgang Sippl, Christoph Ritter & Andreas Hilgeroth
Pages: 271-276
Published online: 18 Jan 2017
AbstractforDiscovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R | Full Text | References | PDF (765.8 KB)
  • 1686 Views
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Research Article

Article
Inhibition behaviours of some phenolic acids on rat kidney aldose reductase enzyme: an in vitro study
Zuhal Alim, Namik Kilinç, Bülent Şengül & Şükrü Beydemir
Pages: 277-284
Published online: 22 Jan 2017
AbstractforInhibition behaviours of some phenolic acids on rat kidney aldose reductase enzyme: an in vitro study | Full Text | References | PDF (883.9 KB)
  • 2557 Views
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Open Access
Article
Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors
Fatih Sonmez, Belma Zengin Kurt, Isil Gazioglu, Livia Basile, Aydan Dag, Valentina Cappello, Tiziana Ginex, Mustafa Kucukislamoglu & Salvatore Guccione
Pages: 285-297
Published online: 18 Jan 2017
AbstractforDesign, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors | Full Text | References | PDF (2.8 MB) | Supplemental
  • 4252 Views
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Open Access
Article
α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives
Jelena B. Popović-Djordjević, Ivana I. Jevtić, Nadja Dj Grozdanić, Sandra B. Šegan, Mario V. Zlatović, Milovan D. Ivanović & Tatjana P. Stanojković
Pages: 298-303
Published online: 19 Jan 2017
Abstractforα-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives | Full Text | References | PDF (656.8 KB)
  • 2113 Views
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Original Article

Article
Inhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives
Francesco Saccoliti, Gabriella Angiulli, Giovanni Pupo, Luca Pescatori, Valentina Noemi Madia, Antonella Messore, Gianni Colotti, Annarita Fiorillo, Luigi Scipione, Marina Gramiccia, Trentina Di Muccio, Roberto Di Santo, Roberta Costi & Andrea Ilari
Pages: 304-310
Published online: 18 Jan 2017
AbstractforInhibition of Leishmania infantum trypanothione reductase by diaryl sulfide derivatives | Full Text | References | PDF (1.6 MB)
  • 2720 Views
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Research Article

Article
Investigation of PDE5/PDE6 and PDE5/PDE11 selective potent tadalafil-like PDE5 inhibitors using combination of molecular modeling approaches, molecular fingerprint-based virtual screening protocols and structure-based pharmacophore development
Gülru Kayık, Nurcan Ş. Tüzün & Serdar Durdagi
Pages: 311-330
Published online: 02 Feb 2017
AbstractforInvestigation of PDE5/PDE6 and PDE5/PDE11 selective potent tadalafil-like PDE5 inhibitors using combination of molecular modeling approaches, molecular fingerprint-based virtual screening protocols and structure-based pharmacophore development | Full Text | References | PDF (3.1 MB) | Supplemental
  • 5045 Views
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Article
Synthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance
Xiaoyun Lu, Zhang Zhang, Xiaomei Ren, Deping Wang & Ke Ding
Pages: 331-336
Published online: 06 Mar 2017
AbstractforSynthesis and identification of GZD856 as an orally bioavailable Bcr-AblT315I inhibitor overcoming acquired imatinib resistance | Full Text | References | PDF (885.7 KB)
  • 1586 Views
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Article
Methanethiosulfonate derivatives as ligands of the STAT3-SH2 domain
Elena Gabriele, Chiara Ricci, Fiorella Meneghetti, Nicola Ferri, Akira Asai & Anna Sparatore
Pages: 337-344
Published online: 18 Jan 2017
AbstractforMethanethiosulfonate derivatives as ligands of the STAT3-SH2 domain | Full Text | References | PDF (903.5 KB)
  • 1322 Views
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Article
Structure–activity relationships of fraxamoside as an unusual xanthine oxidase inhibitor
Rosa Maria Vitale, Lina Antenucci, Margherita Gavagnin, Gennaro Raimo & Pietro Amodeo
Pages: 345-354
Published online: 18 Jan 2017
AbstractforStructure–activity relationships of fraxamoside as an unusual xanthine oxidase inhibitor | Full Text | References | PDF (1.5 MB)
  • 2032 Views
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Article
The lignicolous fungus Trametes versicolor (L.) Lloyd (1920): a promising natural source of antiradical and AChE inhibitory agents
Ljiljana Janjušević, Maja Karaman, Filip Šibul, Giuseppina Tommonaro, Carmine Iodice, Dragica Jakovljević & Boris Pejin
Pages: 355-362
Published online: 18 Jan 2017
AbstractforThe lignicolous fungus Trametes versicolor (L.) Lloyd (1920): a promising natural source of antiradical and AChE inhibitory agents | Full Text | References | PDF (787.7 KB)
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Short Communication

Rapid Communication
Systemic alkalinisation delays prostate cancer cell progression in TRAMP mice
Simonetta Astigiano, Andrea Puglisi, Luca Mastracci, Stefano Fais & Ottavia Barbieri
Pages: 363-368
Published online: 17 Jan 2017
AbstractforSystemic alkalinisation delays prostate cancer cell progression in TRAMP mice | Full Text | References | PDF (734 KB)
  • 2008 Views
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Research Article

Article
Microwave-assisted synthesis and bioevaluation of new sulfonamides
Halise Inci Gul, Cem Yamali, Fatma Yesilyurt, Hiroshi Sakagami, Kaan Kucukoglu, Ilhami Gulcin, Mustafa Gul & Claudiu T. Supuran
Pages: 369-374
Published online: 06 Mar 2017
AbstractforMicrowave-assisted synthesis and bioevaluation of new sulfonamides | Full Text | References | PDF (867.2 KB) | Supplemental
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Original Article

Article
Benzimidazole-based derivatives as privileged scaffold developed for the treatment of the RSV infection: a computational study exploring the potency and cytotoxicity profiles
Elena Cichero, Michele Tonelli, Federica Novelli, Bruno Tasso, Ilenia Delogu, Roberta Loddo, Olga Bruno & Paola Fossa
Pages: 375-402
Published online: 09 Mar 2017
AbstractforBenzimidazole-based derivatives as privileged scaffold developed for the treatment of the RSV infection: a computational study exploring the potency and cytotoxicity profiles | Full Text | References | PDF (20.9 MB) | Supplemental
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Review Article

Review
Skin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors
Thanigaimalai Pillaiyar, Manoj Manickam & Vigneshwaran Namasivayam
Pages: 403-425
Published online: 18 Jan 2017
AbstractforSkin whitening agents: medicinal chemistry perspective of tyrosinase inhibitors | Full Text | References | PDF (2.7 MB)
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Research Article

Article
Expression of heterologous oxalate decarboxylase in HEK293 cells confers protection against oxalate induced oxidative stress as a therapeutic approach for calcium oxalate stone disease
Abhishek Albert, Vidhi Tiwari, Eldho Paul, Divya Ganesan, Mahesh Ayyavu, Ritu Kujur, Sasikumar Ponnusamy, Kathiresan Shanmugam, Luciano Saso & Selvam Govindan Sadasivam
Pages: 426-433
Published online: 24 Jan 2017
AbstractforExpression of heterologous oxalate decarboxylase in HEK293 cells confers protection against oxalate induced oxidative stress as a therapeutic approach for calcium oxalate stone disease | Full Text | References | PDF (1,006.9 KB)
  • 2045 Views
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Article
Probing the druggability of membrane-bound Rab5 by molecular dynamics simulations
Eileen Edler & Matthias Stein
Pages: 434-443
Published online: 16 Jan 2017
AbstractforProbing the druggability of membrane-bound Rab5 by molecular dynamics simulations | Full Text | References | PDF (1.3 MB) | Supplemental
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Short Communication

Rapid Communication
Exploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors
Adriano Mollica, Sveva Pelliccia, Valeria Famiglini, Azzurra Stefanucci, Giorgia Macedonio, Annalisa Chiavaroli, Giustino Orlando, Luigi Brunetti, Claudio Ferrante, Stefano Pieretti, Ettore Novellino, Sandor Benyhe, Ferenc Zador, Anna Erdei, Edina Szucs, Reza Samavati, Szabolcs Dvorácskó, Csaba Tomboly, Rino Ragno, Alexandros Patsilinakos & Romano Silvestri
Pages: 444-451
Published online: 18 Jan 2017
AbstractforExploring the first Rimonabant analog-opioid peptide hybrid compound, as bivalent ligand for CB1 and opioid receptors | Full Text | References | PDF (1.2 MB) | Supplemental
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Research Article

Article
Two approaches to the use of benzo[c][1,2]oxaboroles as active fragments for synthetic transformation of clarithromycin
Gennady B. Lapa, Elena P. Mirchink, Elena B Isakova & Maria N Preobrazhenskaya
Pages: 452-456
Published online: 18 Jan 2017
AbstractforTwo approaches to the use of benzo[c][1,2]oxaboroles as active fragments for synthetic transformation of clarithromycin | Full Text | References | PDF (748.1 KB)
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Article
Synthesis of new pyridothienopyrimidinone derivatives as Pim-1 inhibitors
Bassem H. Naguib, Hala B. El-Nassan & Tamer M. Abdelghany
Pages: 457-467
Published online: 18 Jan 2017
AbstractforSynthesis of new pyridothienopyrimidinone derivatives as Pim-1 inhibitors | Full Text | References | PDF (1.3 MB)
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Article
Purification and biochemical characterization of a novel thermostable serine alkaline protease from Aeribacillus pallidus C10: a potential additive for detergents
Vildan Yildirim, Mustafa Ozkan Baltaci, Ilknur Ozgencli, Melda Sisecioglu, Ahmet Adiguzel & Gulsah Adiguzel
Pages: 468-477
Published online: 18 Jan 2017
AbstractforPurification and biochemical characterization of a novel thermostable serine alkaline protease from Aeribacillus pallidus C10: a potential additive for detergents | Full Text | References | PDF (1.3 MB)
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Article
Disulfiram moderately restores impaired hepatic redox status of rats subchronically exposed to cadmium
Aida Begic, Ana Djuric, Milica Ninkovic, Ivana Stevanovic, Dragan Djurdjevic, Milos Pavlovic, Katarina Jelic, Ana Pantelic, Goran Zebic, Bratislav Dejanovic, Ivan Stanojevic, Danilo Vojvodic, Petar Milosavljevic, Mirjana Djukic & Luciano Saso
Pages: 478-489
Published online: 19 Jan 2017
AbstractforDisulfiram moderately restores impaired hepatic redox status of rats subchronically exposed to cadmium | Full Text | References | PDF (1.3 MB)
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Article
Design of potent fluoro-substituted chalcones as antimicrobial agents
Serdar Burmaoglu, Oztekin Algul, Arzu Gobek, Derya Aktas Anil, Mahmut Ulger, Busra Gul Erturk, Engin Kaplan, Aylin Dogen & Gönül Aslan
Pages: 490-495
Published online: 24 Jan 2017
AbstractforDesign of potent fluoro-substituted chalcones as antimicrobial agents | Full Text | References | PDF (869 KB) | Supplemental
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Original Article

Article
Comparing hydrazine-derived reactive groups as inhibitors of quinone-dependent amine oxidases
Ashley A. Burke, Elizabeth S. Severson, Shreya Mool, Maria J. Solares Bucaro, Frederick T. Greenaway & Charles E. Jakobsche
Pages: 496-503
Published online: 23 Jan 2017
AbstractforComparing hydrazine-derived reactive groups as inhibitors of quinone-dependent amine oxidases | Full Text | References | PDF (1,000.7 KB) | Supplemental
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Article
Evaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors
Ji-Young Park, Heung Joo Yuk, Hyung Won Ryu, Su Hwan Lim, Kyung Su Kim, Ki Hun Park, Young Bae Ryu & Woo Song Lee
Pages: 504-512
Published online: 22 Jan 2017
AbstractforEvaluation of polyphenols from Broussonetia papyrifera as coronavirus protease inhibitors | Full Text | References | PDF (1.3 MB) | Supplemental
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Short Communication

Rapid Communication
N-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors
Naresh Sunduru, Mona Svensson, Mariateresa Cipriano, Sania Marwaha, C. David Andersson, Richard Svensson, Christopher J. Fowler & Mikael Elofsson
Pages: 513-521
Published online: 23 Jan 2017
AbstractforN-aryl 2-aryloxyacetamides as a new class of fatty acid amide hydrolase (FAAH) inhibitors | Full Text | References | PDF (2.1 MB) | Supplemental
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Rapid Communication
Small molecules targeting glycogen synthase kinase 3 as potential drug candidates for the treatment of retinitis pigmentosa
Miguel Marchena, Beatriz Villarejo-Zori, Josefa Zaldivar-Diez, Valle Palomo, Carmen Gil, Catalina Hernández-Sánchez, Ana Martínez & Enrique J. de la Rosa
Pages: 522-526
Published online: 23 Jan 2017
AbstractforSmall molecules targeting glycogen synthase kinase 3 as potential drug candidates for the treatment of retinitis pigmentosa | Full Text | References | PDF (809.4 KB)
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Original Article

Article
Design, synthesis and biological evaluation of novel hydroxy-phenyl-1H-benzimidazoles as radical scavengers and UV-protective agents
Alessia Bino, Anna Baldisserotto, Emanuela Scalambra, Valeria Dissette, Daniela Ester Vedaldi, Alessia Salvador, Elisa Durini, Stefano Manfredini & Silvia Vertuani
Pages: 527-537
Published online: 23 Jan 2017
AbstractforDesign, synthesis and biological evaluation of novel hydroxy-phenyl-1H-benzimidazoles as radical scavengers and UV-protective agents | Full Text | References | PDF (1 MB)
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Research Article

Article
pH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models
Federica Rinaldi, Elena Del Favero, Valeria Rondelli, Stefano Pieretti, Alessia Bogni, Jessica Ponti, François Rossi, Luisa Di Marzio, Donatella Paolino, Carlotta Marianecci & Maria Carafa
Pages: 538-546
Published online: 23 Jan 2017
AbstractforpH-sensitive niosomes: Effects on cytotoxicity and on inflammation and pain in murine models | Full Text | References | PDF (1 MB) | Supplemental
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Article
Design, synthesis and antimalarial activity of novel bis{N-[(pyrrolo[1,2-a]quinoxalin-4-yl)benzyl]-3-aminopropyl}amine derivatives
Jean Guillon, Anita Cohen, Nassima Meriem Gueddouda, Rabindra Nath Das, Stéphane Moreau, Luisa Ronga, Solène Savrimoutou, Louise Basmaciyan, Alix Monnier, Myriam Monget, Sandra Rubio, Timothée Garnerin, Nadine Azas, Jean-Louis Mergny, Catherine Mullié & Pascal Sonnet
Pages: 547-563
Published online: 23 Jan 2017
AbstractforDesign, synthesis and antimalarial activity of novel bis{N-[(pyrrolo[1,2-a]quinoxalin-4-yl)benzyl]-3-aminopropyl}amine derivatives | Full Text | References | PDF (1.6 MB)
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Article
A mechanistic kinetic description of lactate dehydrogenase elucidating cancer diagnosis and inhibitor evaluation
Peifeng Tang, Jianlin Xu, Christopher L. Oliveira, Zheng Jian Li & Shijie Liu
Pages: 564-571
Published online: 24 Jan 2017
AbstractforA mechanistic kinetic description of lactate dehydrogenase elucidating cancer diagnosis and inhibitor evaluation | Full Text | References | PDF (962.2 KB)
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Review Article

Review
Novel multitarget-directed tacrine derivatives as potential candidates for the treatment of Alzheimer’s disease
Wen-Yu Wu, Yu-Chen Dai, Nian-Guang Li, Ze-Xi Dong, Ting Gu, Zhi-Hao Shi, Xin Xue, Yu-Ping Tang & Jin-Ao Duan
Pages: 572-587
Published online: 29 Jan 2017
AbstractforNovel multitarget-directed tacrine derivatives as potential candidates for the treatment of Alzheimer’s disease | Full Text | References | PDF (1.7 MB)
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Research Article

Article
New arylsparteine derivatives as positive inotropic drugs
Vito Boido, Marcella Ercoli, Michele Tonelli, Federica Novelli, Bruno Tasso, Fabio Sparatore, Elena Cichero, Paola Fossa, Paola Dorigo & Guglielmina Froldi
Pages: 588-599
Published online: 29 Jan 2017
AbstractforNew arylsparteine derivatives as positive inotropic drugs | Full Text | References | PDF (1.3 MB)
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Article
Synthesis and in vitro anti-proliferative activity of some novel isatins conjugated with quinazoline/phthalazine hydrazines against triple-negative breast cancer MDA-MB-231 cells as apoptosis-inducing agents
Wagdy M. Eldehna, Hadia Almahli, Ghada H. Al-Ansary, Hazem A. Ghabbour, Mohamed H. Aly, Omnia E. Ismael, Abdullah Al-Dhfyan & Hatem A. Abdel-Aziz
Pages: 600-613
Published online: 08 Feb 2017
AbstractforSynthesis and in vitro anti-proliferative activity of some novel isatins conjugated with quinazoline/phthalazine hydrazines against triple-negative breast cancer MDA-MB-231 cells as apoptosis-inducing agents | Full Text | References | PDF (1.6 MB)
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Article
Metabolite profiling of ascidian Styela plicata using LC–MS with multivariate statistical analysis and their antitumor activity
Satheesh Kumar Palanisamy, Daniela Trisciuoglio, Clemens Zwergel, Donatella Del Bufalo & Antonello Mai
Pages: 614-623
Published online: 24 Feb 2017
AbstractforMetabolite profiling of ascidian Styela plicata using LC–MS with multivariate statistical analysis and their antitumor activity | Full Text | References | PDF (1.7 MB) | Supplemental
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Article
A potent peptide as adiponectin receptor 1 agonist to against fibrosis
Lingman Ma, Zhen Zhang, Xiaowen Xue, Yumeng Wan, Boping Ye & Kejiang Lin
Pages: 624-631
Published online: 06 Mar 2017
AbstractforA potent peptide as adiponectin receptor 1 agonist to against fibrosis | Full Text | References | PDF (1.2 MB)
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Article
Biochemical characterization of the native α-carbonic anhydrase purified from the mantle of the Mediterranean mussel, Mytilus galloprovincialis
Rosa Perfetto, Sonia Del Prete, Daniela Vullo, Giovanni Sansone, Carmela Barone, Mosè Rossi, Claudiu T. Supuran & Clemente Capasso
Pages: 632-639
Published online: 23 Feb 2017
AbstractforBiochemical characterization of the native α-carbonic anhydrase purified from the mantle of the Mediterranean mussel, Mytilus galloprovincialis | Full Text | References | PDF (893.6 KB)
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Article
A new colorimetric DPPH• scavenging activity method with no need for a spectrophotometer applied on synthetic and natural antioxidants and medicinal herbs
Zeynep Akar, Murat Küçük & Hacer Doğan
Pages: 640-647
Published online: 06 Mar 2017
AbstractforA new colorimetric DPPH• scavenging activity method with no need for a spectrophotometer applied on synthetic and natural antioxidants and medicinal herbs | Full Text | References | PDF (1.1 MB)
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Article
Acridine Orange/exosomes increase the delivery and the effectiveness of Acridine Orange in human melanoma cells: A new prototype for theranostics of tumors
Elisabetta Iessi, Mariantonia Logozzi, Luana Lugini, Tommaso Azzarito, Cristina Federici, Enrico Pierluigi Spugnini, Davide Mizzoni, Rossella Di Raimo, Daniela F. Angelini, Luca Battistini, Serena Cecchetti & Stefano Fais
Pages: 648-657
Published online: 06 Mar 2017
AbstractforAcridine Orange/exosomes increase the delivery and the effectiveness of Acridine Orange in human melanoma cells: A new prototype for theranostics of tumors | Full Text | References | PDF (1.1 MB)
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Erratum

Correction
Correction to: Synthesis, antitumor screening and cell cycle analysis of novel benzothieno[3,2-b]pyran derivatives
Page: 658
Published online: 25 Oct 2016
CitationforCorrection to: Synthesis, antitumor screening and cell cycle analysis of novel benzothieno[3,2-b]pyran derivatives | Full Text | PDF (123.1 KB)
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Research Article

Article
Pharmacophore-based design and discovery of (−)-meptazinol carbamates as dual modulators of cholinesterase and amyloidogenesis
Qiong Xie, Zhaoxi Zheng, Biyun Shao, Wei Fu, Zheng Xia, Wei Li, Jian Sun, Wei Zheng, Weiwei Zhang, Wei Sheng, Qihong Zhang, Hongzhuan Chen, Hao Wang & Zhuibai Qiu
Pages: 659-671
Published online: 08 Mar 2017
AbstractforPharmacophore-based design and discovery of (−)-meptazinol carbamates as dual modulators of cholinesterase and amyloidogenesis | Full Text | References | PDF (1.7 MB)
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Article
Differential representation of liver proteins in obese human subjects suggests novel biomarkers and promising targets for drug development in obesity
Simonetta Caira, Antonio Iannelli, Rosaria Sciarrillo, Gianluca Picariello, Giovanni Renzone, Andrea Scaloni & Pietro Addeo
Pages: 672-682
Published online: 08 Mar 2017
AbstractforDifferential representation of liver proteins in obese human subjects suggests novel biomarkers and promising targets for drug development in obesity | Full Text | References | PDF (1.1 MB) | Supplemental
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Review Article

Review
Brucella suis carbonic anhydrases and their inhibitors: Towards alternative antibiotics?
Stephan Köhler, Safia Ouahrani-Bettache & Jean-Yves Winum
Pages: 683-687
Published online: 08 Mar 2017
AbstractforBrucella suis carbonic anhydrases and their inhibitors: Towards alternative antibiotics? | Full Text | References | PDF (607.6 KB)
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Original Article

Article
3D QSAR studies, pharmacophore modeling, and virtual screening of diarylpyrazole–benzenesulfonamide derivatives as a template to obtain new inhibitors, using human carbonic anhydrase II as a model protein
Yeganeh Entezari Heravi, Hassan Sereshti, Ali Akbar Saboury, Jahan Ghasemi, Marzieh Amirmostofian & Claudiu T. Supuran
Pages: 688-700
Published online: 19 Mar 2017
Abstractfor3D QSAR studies, pharmacophore modeling, and virtual screening of diarylpyrazole–benzenesulfonamide derivatives as a template to obtain new inhibitors, using human carbonic anhydrase II as a model protein | Full Text | References | PDF (1.7 MB) | Supplemental
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Research Article

Article
Synthesis of an acridine orange sulfonamide derivative with potent carbonic anhydrase IX inhibitory action
Marco Bragagni, Fabrizio Carta, Sameh M. Osman, Zeid AlOthman & Claudiu T. Supuran
Pages: 701-706
Published online: 23 Mar 2017
AbstractforSynthesis of an acridine orange sulfonamide derivative with potent carbonic anhydrase IX inhibitory action | Full Text | References | PDF (692.8 KB)
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Article
Hyperbaric oxygen therapy modulates serum OPG/RANKL in femoral head necrosis patients
Giuliano Vezzani, Silvia Quartesan, Pasqua Cancellara, Enrico Camporesi, Devanand Mangar, Thomas Bernasek, Prachiti Dalvi, Zhongjin Yang, Antonio Paoli, Alex Rizzato & Gerardo Bosco
Pages: 707-711
Published online: 07 Apr 2017
AbstractforHyperbaric oxygen therapy modulates serum OPG/RANKL in femoral head necrosis patients | Full Text | References | PDF (523.6 KB)
  • 2459 Views
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Article
Effects of NS2B-NS3 protease and furin inhibition on West Nile and Dengue virus replication
Jenny Kouretova, M. Zouhir Hammamy, Anton Epp, Kornelia Hardes, Stephanie Kallis, Linlin Zhang, Rolf Hilgenfeld, Ralf Bartenschlager & Torsten Steinmetzer
Pages: 712-721
Published online: 07 Apr 2017
AbstractforEffects of NS2B-NS3 protease and furin inhibition on West Nile and Dengue virus replication | Full Text | References | PDF (1.4 MB)
  • 3086 Views
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Article
Design, synthesis and evaluation of 18F-labeled cationic carbonic anhydrase IX inhibitors for PET imaging
Zhengxing Zhang, Joseph Lau, Chengcheng Zhang, Nadine Colpo, Alessio Nocentini, Claudiu T. Supuran, François Bénard & Kuo-Shyan Lin
Pages: 722-730
Published online: 07 Apr 2017
AbstractforDesign, synthesis and evaluation of 18F-labeled cationic carbonic anhydrase IX inhibitors for PET imaging | Full Text | References | PDF (1,020.9 KB)
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Retraction

Retraction
Statement of Retraction
Page: 731
Published online: 20 Apr 2017
CitationforStatement of Retraction | Full Text | PDF (142.6 KB)
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Research Article

Article
Design, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents
Hülya Karaca Gençer, Ulviye Acar Çevik, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Serkan Levent, Özlem Atlı, Sinem Ilgın, Yusuf Özkay & Zafer Asım Kaplancıklı
Pages: 732-745
Published online: 16 Apr 2017
First Page PreviewforDesign, synthesis, and evaluation of novel 2-phenylpropionic acid derivatives as dual COX inhibitory-antibacterial agents | Full Text | References | PDF (1.7 MB)
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Research Paper

Article
Synthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives
Simone Carradori, Daniela Secci, Bruna Bizzarri, Paola Chimenti, Celeste De Monte, Paolo Guglielmi, Cristina Campestre, Daniela Rivanera, Claudia Bordón & Lorraine Jones-Brando
Pages: 746-758
Published online: 24 May 2017
AbstractforSynthesis and biological evaluation of anti-Toxoplasma gondii activity of a novel scaffold of thiazolidinone derivatives | Full Text | References | PDF (3.1 MB) | Supplemental
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Article
Production and covalent immobilisation of the recombinant bacterial carbonic anhydrase (SspCA) onto magnetic nanoparticles
Rosa Perfetto, Sonia Del Prete, Daniela Vullo, Giovanni Sansone, Carmela M.A. Barone, Mosè Rossi, Claudiu T. Supuran & Clemente Capasso
Pages: 759-766
Published online: 12 May 2017
AbstractforProduction and covalent immobilisation of the recombinant bacterial carbonic anhydrase (SspCA) onto magnetic nanoparticles | Full Text | References | PDF (960.3 KB)
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Article
3H-1,2-benzoxathiepine 2,2-dioxides: a new class of isoform-selective carbonic anhydrase inhibitors
Aleksandrs Pustenko, Dmitrijs Stepanovs, Raivis Žalubovskis, Daniela Vullo, Andris Kazaks, Janis Leitans, Kaspars Tars & Claudiu T. Supuran
Pages: 767-775
Published online: 24 May 2017
Abstractfor3H-1,2-benzoxathiepine 2,2-dioxides: a new class of isoform-selective carbonic anhydrase inhibitors | Full Text | References | PDF (1.8 MB)
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Research Article

Article
Design, synthesis and evaluation of novel cinnamic acid derivatives bearing N-benzyl pyridinium moiety as multifunctional cholinesterase inhibitors for Alzheimer’s disease
Jin-Shuai Lan, Jian-Wei Hou, Yun Liu, Yue Ding, Yong Zhang, Ling Li & Tong Zhang
Pages: 776-788
Published online: 06 Jun 2017
AbstractforDesign, synthesis and evaluation of novel cinnamic acid derivatives bearing N-benzyl pyridinium moiety as multifunctional cholinesterase inhibitors for Alzheimer’s disease | Full Text | References | PDF (1.5 MB)
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Research Paper

Article
Resorcinol-, catechol- and saligenin-based bronchodilating β2-agonists as inhibitors of human cholinesterase activity
Anita Bosak, Anamarija Knežević, Ivana Gazić Smilović, Goran Šinko & Zrinka Kovarik
Pages: 789-797
Published online: 02 Jun 2017
AbstractforResorcinol-, catechol- and saligenin-based bronchodilating β2-agonists as inhibitors of human cholinesterase activity | Full Text | References | PDF (1.2 MB) | Supplemental
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Article
Inhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties
Daniela De Vita, Andrea Angeli, Fabiana Pandolfi, Martina Bortolami, Roberta Costi, Roberto Di Santo, Elisabetta Suffredini, Mariangela Ceruso, Sonia Del Prete, Clemente Capasso, Luigi Scipione & Claudiu T. Supuran
Pages: 798-804
Published online: 01 Jun 2017
AbstractforInhibition of the α-carbonic anhydrase from Vibrio cholerae with amides and sulfonamides incorporating imidazole moieties | Full Text | References | PDF (1.8 MB)
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Article
Novel tetrazole and cyanamide derivatives as inhibitors of cyclooxygenase-2 enzyme: design, synthesis, anti-inflammatory evaluation, ulcerogenic liability and docking study
Phoebe F. Lamie, John N. Philoppes, Amany A. Azouz & Nesreen M. Safwat
Pages: 805-820
Published online: 06 Jun 2017
AbstractforNovel tetrazole and cyanamide derivatives as inhibitors of cyclooxygenase-2 enzyme: design, synthesis, anti-inflammatory evaluation, ulcerogenic liability and docking study | Full Text | References | PDF (2 MB)
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Reasearch Paper

Article
Isoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors
Claudia Vergelli, Igor A. Schepetkin, Letizia Crocetti, Antonella Iacovone, Maria Paola Giovannoni, Gabriella Guerrini, Andrei I. Khlebnikov, Samuele Ciattini, Giovanna Ciciani & Mark T. Quinn
Pages: 821-831
Published online: 14 Jun 2017
AbstractforIsoxazol-5(2H)-one: a new scaffold for potent human neutrophil elastase (HNE) inhibitors | Full Text | References | PDF (1.5 MB) | Supplemental
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Original Article

Article
β-CA-specific inhibitor dithiocarbamate Fc14–584B: a novel antimycobacterial agent with potential to treat drug-resistant tuberculosis
Ashok Aspatwar, Milka Hammarén, Sanni Koskinen, Bruno Luukinen, Harlan Barker, Fabrizio Carta, Claudiu T. Supuran, Mataleena Parikka & Seppo Parkkila
Pages: 832-840
Published online: 20 Jun 2017
Abstractforβ-CA-specific inhibitor dithiocarbamate Fc14–584B: a novel antimycobacterial agent with potential to treat drug-resistant tuberculosis | Full Text | References | PDF (1.2 MB) | Supplemental
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Research Paper

Article
Advances in new psychoactive substances identification: the U.R.I.To.N. Consortium
Elisabetta Bertol, Fabio Vaiano, Francesco Mari, Maria Grazia Di Milia, Silvia Bua, Claudiu T. Supuran & Fabrizio Carta
Pages: 841-849
Published online: 20 Jun 2017
AbstractforAdvances in new psychoactive substances identification: the U.R.I.To.N. Consortium | Full Text | References | PDF (1.3 MB) | Supplemental
  • 2553 Views
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Article
Design, synthesis and evaluation of 2-aryl benzoxazoles as promising hit for the A2A receptor
Romain Duroux, Nicolas Renault, Joana Esteves Cuelho, Laurence Agouridas, David Blum, Luisa V. Lopes, Patricia Melnyk & Saïd Yous
Pages: 850-864
Published online: 29 Jun 2017
AbstractforDesign, synthesis and evaluation of 2-aryl benzoxazoles as promising hit for the A2A receptor | Full Text | References | PDF (1.7 MB) | Supplemental
  • 1727 Views
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Original Article

Article
Naphthoquinone amino acid derivatives, synthesis and biological activity as proteasome inhibitors
Mauro Marastoni, Claudio Trapella, Alessandra Scotti, Anna Fantinati, Valeria Ferretti, Erika Marzola, Gallerani Eleonora, Riccardo Gavioli & Delia Preti
Pages: 865-877
Published online: 28 Jun 2017
AbstractforNaphthoquinone amino acid derivatives, synthesis and biological activity as proteasome inhibitors | Full Text | References | PDF (1.7 MB) | Supplemental
  • 1781 Views
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Article
Syntheses and evaluation of multicaulin and miltirone-like compounds as antituberculosis agents
Serdar Burmaoğlu, Hatice Seçinti, Erkan Mozioğlu, Ahmet C. Gören, Ramazan Altundaş & Hasan Seçen
Pages: 878-884
Published online: 29 Jun 2017
AbstractforSyntheses and evaluation of multicaulin and miltirone-like compounds as antituberculosis agents | Full Text | References | PDF (1,016.2 KB) | Supplemental
  • 1257 Views
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Article
Carbonic anhydrase I, II, IV and IX inhibition with a series of 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives
Murat Bozdag, Silvia Bua, Sameh M. Osman, Zeid AlOthman & Claudiu T. Supuran
Pages: 885-892
Published online: 23 Jun 2017
AbstractforCarbonic anhydrase I, II, IV and IX inhibition with a series of 7-amino-3,4-dihydroquinolin-2(1H)-one derivatives | Full Text | References | PDF (765.4 KB)
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Article
VEGFR-2 inhibitors and apoptosis inducers: synthesis and molecular design of new benzo[g]quinazolin bearing benzenesulfonamide moiety
Mostafa M. Ghorab, Mansour S. Alsaid, Aiten M. Soliman & Fatma A. Ragab
Pages: 893-907
Published online: 29 Jun 2017
First Page PreviewforVEGFR-2 inhibitors and apoptosis inducers: synthesis and molecular design of new benzo[g]quinazolin bearing benzenesulfonamide moiety | Full Text | References | PDF (2.2 MB) | Supplemental
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Review

Review
Natural extracellular nanovesicles and photodynamic molecules: is there a future for drug delivery?
Katsuyuki Kusuzaki, Takao Matsubara, Hiroaki Murata, Mariantonia Logozzi, Elisabetta Iessi, Rossella Di Raimo, Fabrizio Carta, Claudiu T. Supuran & Stefano Fais
Pages: 908-916
Published online: 14 Jul 2017
AbstractforNatural extracellular nanovesicles and photodynamic molecules: is there a future for drug delivery? | Full Text | References | PDF (918.1 KB)
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Original Article

Article
Beta-lactamase database (BLDB) – structure and function
Thierry Naas, Saoussen Oueslati, Rémy A. Bonnin, Maria Laura Dabos, Agustin Zavala, Laurent Dortet, Pascal Retailleau & Bogdan I. Iorga
Pages: 917-919
Published online: 19 Jul 2017
AbstractforBeta-lactamase database (BLDB) – structure and function | Full Text | References | PDF (1 MB) | Supplemental
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Research Article

Article
Primary mono- and bis-sulfonamides obtained via regiospecific sulfochlorination of N-arylpyrazoles: inhibition profile against a panel of human carbonic anhydrases
Mikhail Krasavin, Mikhail Korsakov, Oksana Ronzhina, Tiziano Tuccinardi, Stanislav Kalinin, Muhammet Tanç & Claudiu T. Supuran
Pages: 920-934
Published online: 18 Jul 2017
AbstractforPrimary mono- and bis-sulfonamides obtained via regiospecific sulfochlorination of N-arylpyrazoles: inhibition profile against a panel of human carbonic anhydrases | Full Text | References | PDF (4.5 MB)
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Open Access
Article
Synthesis, anticancer and apoptosis-inducing activities of quinazoline–isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies
Adel S. El-Azab, Abdullah Al-Dhfyan, Alaa A.-M. Abdel-Aziz, Laila A. Abou-Zeid, Hamad M. Alkahtani, Abdulrahman M. Al-Obaid & Manal A. Al-Gendy
Pages: 935-944
Published online: 18 Jul 2017
AbstractforSynthesis, anticancer and apoptosis-inducing activities of quinazoline–isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies | Full Text | References | PDF (1.3 MB)
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Research Paper

Article
Rosmarinic acid prevents fibrillization and diminishes vibrational modes associated to β sheet in tau protein linked to Alzheimer’s disease
Alberto Cornejo, Felipe Aguilar Sandoval, Leonardo Caballero, Luis Machuca, Patricio Muñoz, Julio Caballero, George Perry, Alejandro Ardiles, Carlos Areche & Francisco Melo
Pages: 945-953
Published online: 13 Jul 2017
AbstractforRosmarinic acid prevents fibrillization and diminishes vibrational modes associated to β sheet in tau protein linked to Alzheimer’s disease | Full Text | References | PDF (1.4 MB)
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Short Communication

Rapid Communication
Design and synthesis of a novel photoaffinity probe for labelling EGF receptor tyrosine kinases
You-Guang Zheng, Xiao-Qing Wu, Jun Su, Ping Jiang, Liang Xu, Jian Gao, Bin Cai & Min Ji
Pages: 954-959
Published online: 18 Jul 2017
AbstractforDesign and synthesis of a novel photoaffinity probe for labelling EGF receptor tyrosine kinases | Full Text | References | PDF (982.7 KB) | Supplemental
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Research Paper

Article
Subnanomolar indazole-5-carboxamide inhibitors of monoamine oxidase B (MAO-B) continued: indications of iron binding, experimental evidence for optimised solubility and brain penetration
Nikolay T. Tzvetkov & Liudmil Antonov
Pages: 960-967
Published online: 20 Jul 2017
AbstractforSubnanomolar indazole-5-carboxamide inhibitors of monoamine oxidase B (MAO-B) continued: indications of iron binding, experimental evidence for optimised solubility and brain penetration | Full Text | References | PDF (1.1 MB) | Supplemental
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Article
Discovery of novel isoflavone derivatives as AChE/BuChE dual-targeted inhibitors: synthesis, biological evaluation and molecular modelling
Bo Feng, Xinpeng Li, Jie Xia & Song Wu
Pages: 968-977
Published online: 18 Jul 2017
AbstractforDiscovery of novel isoflavone derivatives as AChE/BuChE dual-targeted inhibitors: synthesis, biological evaluation and molecular modelling | Full Text | References | PDF (2.1 MB) | Supplemental
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Open Access
Article
Kinetic study on the inhibition of xanthine oxidase by acylated derivatives of flavonoids synthesised enzymatically
Maria Elisa Melo Branco de Araújo, Yollanda Edwirges Moreira Franco, Thiago Grando Alberto, Marcia Cristina Fernandes Messias, Camila Wielewski Leme, Alexandra Christine Helena Frankland Sawaya & Patricia de Oliveira Carvalho
Pages: 978-985
Published online: 18 Jul 2017
AbstractforKinetic study on the inhibition of xanthine oxidase by acylated derivatives of flavonoids synthesised enzymatically | Full Text | References | PDF (848.3 KB)
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Short Communication

Rapid Communication
Cancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo[3,2-a]benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation
Ghada H. Al-Ansary, Wagdy M. Eldehna, Hazem A. Ghabbour, Sara T. A. Al-Rashood, Khalid A. Al-Rashood, Radwa A. Eladwy, Abdullah Al-Dhfyan, Maha M. Kabil & Hatem A. Abdel-Aziz
Pages: 986-991
Published online: 20 Jul 2017
AbstractforCancer stem cells CD133 inhibition and cytotoxicity of certain 3-phenylthiazolo[3,2-a]benzimidazoles: design, direct synthesis, crystal study and in vitro biological evaluation | Full Text | References | PDF (869.3 KB) | Supplemental
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Research Paper

Article
Design and synthesis of benzopyran-based inhibitors of the hypoxia-inducible factor-1 pathway with improved water solubility
Jalisa H. Ferguson, Zeus De Los Santos, Saroja N. Devi, Stefan Kaluz, Erwin G. Van Meir, Sarah K. Zingales & Binghe Wang
Pages: 992-1001
Published online: 02 Aug 2017
AbstractforDesign and synthesis of benzopyran-based inhibitors of the hypoxia-inducible factor-1 pathway with improved water solubility | Full Text | References | PDF (2.1 MB) | Supplemental
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Article
Insights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations
Giuseppina De Simone, Emma Langella, Davide Esposito, Claudiu T. Supuran, Simona Maria Monti, Jean-Yves Winum & Vincenzo Alterio
Pages: 1002-1011
Published online: 24 Jul 2017
AbstractforInsights into the binding mode of sulphamates and sulphamides to hCA II: crystallographic studies and binding free energy calculations | Full Text | References | PDF (2.9 MB)
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Article
New sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors
Elena Gabriele, Dario Brambilla, Chiara Ricci, Luca Regazzoni, Kyoko Taguchi, Nicola Ferri, Akira Asai & Anna Sparatore
Pages: 1012-1028
Published online: 25 Jul 2017
AbstractforNew sulfurated derivatives of cinnamic acids and rosmaricine as inhibitors of STAT3 and NF-κB transcription factors | Full Text | References | PDF (1.8 MB)
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Original Article

Article
Cloning, expression and purification of the α-carbonic anhydrase from the mantle of the Mediterranean mussel, Mytilus galloprovincialis
Rosa Perfetto, Sonia Del Prete, Daniela Vullo, Vincenzo Carginale, Giovanni Sansone, Carmela M. A. Barone, Mosè Rossi, Fatmah A. S. Alasmary, Sameh M. Osman, Zeid AlOthman, Claudiu T. Supuran & Clemente Capasso
Pages: 1029-1035
Published online: 25 Jul 2017
AbstractforCloning, expression and purification of the α-carbonic anhydrase from the mantle of the Mediterranean mussel, Mytilus galloprovincialis | Full Text | References | PDF (1 MB)
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Research paper

Article
Water permeability is a measure of severity in acute appendicitis
Nicola Pini, Viktoria A. Pfeifle, Urs Kym, Simone Keck, Virginie Galati, Stefan Holland-Cunz & Stephanie J. Gros
Pages: 1036-1041
Published online: 01 Aug 2017
AbstractforWater permeability is a measure of severity in acute appendicitis | Full Text | References | PDF (782.3 KB)
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Research Paper

Article
Synthesis, biological activity and multiscale molecular modeling studies for coumaryl-carboxamide derivatives as selective carbonic anhydrase IX inhibitors
Belma Zengin Kurt, Fatih Sonmez, Serdar Durdagi, Busecan Aksoydan, Ramin Ekhteiari Salmas, Andrea Angeli, Mustafa Kucukislamoglu & Claudiu T. Supuran
Pages: 1042-1052
Published online: 04 Aug 2017
AbstractforSynthesis, biological activity and multiscale molecular modeling studies for coumaryl-carboxamide derivatives as selective carbonic anhydrase IX inhibitors | Full Text | References | PDF (2.2 MB) | Supplemental
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Article
Analysis of imidazoles and triazoles in biological samples after MicroExtraction by packed sorbent
Cristina Campestre, Marcello Locatelli, Paolo Guglielmi, Elisa De Luca, Giuseppe Bellagamba, Sergio Menta, Gokhan Zengin, Christian Celia, Luisa Di Marzio & Simone Carradori
Pages: 1053-1063
Published online: 04 Aug 2017
AbstractforAnalysis of imidazoles and triazoles in biological samples after MicroExtraction by packed sorbent | Full Text | References | PDF (1.4 MB) | Supplemental
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Open Access
Article
Inhibition of the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa with monothiocarbamates
Alessio Nocentini, Daniela Vullo, Sonia Del Prete, Sameh M. Osman, Fatmah A.S. Alasmary, Zeid AlOthman, Clemente Capasso, Fabrizio Carta, Paola Gratteri & Claudiu T. Supuran
Pages: 1064-1070
Published online: 02 Aug 2017
AbstractforInhibition of the β-carbonic anhydrase from the dandruff-producing fungus Malassezia globosa with monothiocarbamates | Full Text | References | PDF (1 MB)
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Article
Synthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides
Morteza Abdoli, Andrea Angeli, Murat Bozdag, Fabrizio Carta, Ali Kakanejadifard, Hamid Saeidian & Claudiu T. Supuran
Pages: 1071-1078
Published online: 28 Jul 2017
AbstractforSynthesis and carbonic anhydrase I, II, VII, and IX inhibition studies with a series of benzo[d]thiazole-5- and 6-sulfonamides | Full Text | References | PDF (855.7 KB)
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Research Article

Article
Quantitative assessment of specific carbonic anhydrase inhibitors effect on hypoxic cells using electrical impedance assays
Luciana Stanica, Mihaela Gheorghiu, Miruna Stan, Cristina Polonschii, Sorin David, Dumitru Bratu, Anca Dinischiotu, Claudiu T. Supuran & Eugen Gheorghiu
Pages: 1079-1090
Published online: 07 Aug 2017
AbstractforQuantitative assessment of specific carbonic anhydrase inhibitors effect on hypoxic cells using electrical impedance assays | Full Text | References | PDF (1.5 MB) | Supplemental
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Research Paper

Article
Inhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities
Sveva Pelliccia, Yu-Hsuan Wu, Antonio Coluccia, Giuseppe La Regina, Chin-Kai Tseng, Valeria Famiglini, Domiziana Masci, John Hiscott, Jin-Ching Lee & Romano Silvestri
Pages: 1091-1101
Published online: 04 Aug 2017
AbstractforInhibition of dengue virus replication by novel inhibitors of RNA-dependent RNA polymerase and protease activities | Full Text | References | PDF (1.5 MB)
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Article
Allosteric inhibition of carnosinase (CN1) by inducing a conformational shift
Verena Peters, Claus P. Schmitt, Tim Weigand, Kristina Klingbeil, Christian Thiel, Antje van den Berg, Vittorio Calabrese, Peter Nawroth, Thomas Fleming, Elisabete Forsberg, Andreas H. Wagner, Markus Hecker & Giulio Vistoli
Pages: 1102-1110
Published online: 04 Aug 2017
AbstractforAllosteric inhibition of carnosinase (CN1) by inducing a conformational shift | Full Text | References | PDF (1.3 MB)
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Article
Synthesis and biological evaluation of novel 7-hydroxy-4-phenylchromen-2-one–linked to triazole moieties as potent cytotoxic agents
Chuan-Feng Liu, Qing-Kun Shen, Jia-Jun Li, Yu-Shun Tian & Zheshan Quan
Pages: 1111-1119
Published online: 09 Aug 2017
AbstractforSynthesis and biological evaluation of novel 7-hydroxy-4-phenylchromen-2-one–linked to triazole moieties as potent cytotoxic agents | Full Text | References | PDF (981.4 KB)
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Article
A one-step procedure for immobilising the thermostable carbonic anhydrase (SspCA) on the surface membrane of Escherichia coli
Sonia Del Prete, Rosa Perfetto, Mosè Rossi, Fatmah A. S. Alasmary, Sameh M. Osman, Zeid AlOthman, Claudiu T. Supuran & Clemente Capasso
Pages: 1120-1128
Published online: 09 Aug 2017
AbstractforA one-step procedure for immobilising the thermostable carbonic anhydrase (SspCA) on the surface membrane of Escherichia coli | Full Text | References | PDF (964 KB)
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Short Communication

Rapid Communication
Multicomponent synthesis of some new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro anti-proliferative activity against CaSki, MDA-MB-231 and SK-Lu-1 tumour cells as apoptosis inducing agents without necrosis
Sujay Laskar, Luis Sánchez-Sánchez, Manuel López-Ortiz, Hugo López-Muñoz, María L. Escobar-Sánchez, Arturo T. Sánchez & Ignacio Regla
Pages: 1129-1135
Published online: 03 Sep 2017
AbstractforMulticomponent synthesis of some new (1S,4S)-2,5-diazabicyclo[2.2.1]heptane-dithiocarbamates and their in vitro anti-proliferative activity against CaSki, MDA-MB-231 and SK-Lu-1 tumour cells as apoptosis inducing agents without necrosis | Full Text | References | PDF (965.5 KB)
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Research Paper

Article
Inhibition of human cytochromes P450 2A6 and 2A13 by flavonoids, acetylenic thiophenes and sesquiterpene lactones from Pluchea indica and Vernonia cinerea
Supattra Boonruang, Khanistha Prakobsri, Phisit Pouyfung, Ekaruth Srisook, Aruna Prasopthum, Pornpimol Rongnoparut & Songklod Sarapusit
Pages: 1136-1142
Published online: 31 Aug 2017
AbstractforInhibition of human cytochromes P450 2A6 and 2A13 by flavonoids, acetylenic thiophenes and sesquiterpene lactones from Pluchea indica and Vernonia cinerea | Full Text | References | PDF (878.3 KB) | Supplemental
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Article
New quinoxalinone inhibitors targeting secreted phospholipase A2 and α-glucosidase
Fatmah A. S. Alasmary, Fatima S. Alnahdi, Abir Ben Bacha, Amr M. El-Araby, Nadine Moubayed, Ahmed M. Alafeefy & Moustafa E. El-Araby
Pages: 1143-1151
Published online: 31 Aug 2017
AbstractforNew quinoxalinone inhibitors targeting secreted phospholipase A2 and α-glucosidase | Full Text | References | PDF (1.2 MB)
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Article
The use of dimethylsulfoxide as a solvent in enzyme inhibition studies: the case of aldose reductase
Livia Misuri, Mario Cappiello, Francesco Balestri, Roberta Moschini, Vito Barracco, Umberto Mura & Antonella Del-Corso
Pages: 1152-1158
Published online: 31 Aug 2017
AbstractforThe use of dimethylsulfoxide as a solvent in enzyme inhibition studies: the case of aldose reductase | Full Text | References | PDF (841.7 KB)
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Article
Novel series of 1,2,4-trioxane derivatives as antimalarial agents
Mithun Rudrapal, Dipak Chetia & Vineeta Singh
Pages: 1159-1173
Published online: 05 Sep 2017
AbstractforNovel series of 1,2,4-trioxane derivatives as antimalarial agents | Full Text | References | PDF (1.8 MB) | Supplemental
  • 2184 Views
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Article
Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors
İlhami Gulçin, Malahat Abbasova, Parham Taslimi, Zübeyir Huyut, Leyla Safarova, Afsun Sujayev, Vagif Farzaliyev, Şükrü Beydemir, Saleh H. Alwasel & Claudiu T. Supuran
Pages: 1174-1182
Published online: 11 Sep 2017
AbstractforSynthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors | Full Text | References | PDF (1.3 MB)
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Short Communication

Rapid Communication
Design, synthesis and biological activity of pyrazinamide derivatives for anti-Mycobacterium tuberculosis
Shiyang Zhou, Shanbin Yang & Gangliang Huang
Pages: 1183-1186
Published online: 04 Sep 2017
AbstractforDesign, synthesis and biological activity of pyrazinamide derivatives for anti-Mycobacterium tuberculosis | Full Text | References | PDF (534.1 KB)
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Research Paper

Article
Synthesis and biological evaluation of benzenesulphonamide-bearing 1,4,5-trisubstituted-1,2,3-triazoles possessing human carbonic anhydrase I, II, IV, and IX inhibitory activity
Rajiv Kumar, Vikas Sharma, Silvia Bua, Claudiu T. Supuran & Pawan K. Sharma
Pages: 1187-1194
Published online: 11 Sep 2017
AbstractforSynthesis and biological evaluation of benzenesulphonamide-bearing 1,4,5-trisubstituted-1,2,3-triazoles possessing human carbonic anhydrase I, II, IV, and IX inhibitory activity | Full Text | References | PDF (833.4 KB)
  • 1500 Views
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Article
Inhibition of protein tyrosine phosphatase (PTP1B) and α-glucosidase by geranylated flavonoids from Paulownia tomentosa
Yeong Hun Song, Zia Uddin, Young Min Jin, Zuopeng Li, Marcus John Curtis-Long, Kwang Dong Kim, Jung Keun Cho & Ki Hun Park
Pages: 1195-1202
Published online: 21 Sep 2017
AbstractforInhibition of protein tyrosine phosphatase (PTP1B) and α-glucosidase by geranylated flavonoids from Paulownia tomentosa | Full Text | References | PDF (851.7 KB) | Supplemental
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Article
Reactive oxygen species inhibit catalytic activity of peptidylarginine deiminase
Dres Damgaard, Mads Emil Bjørn, Peter Østrup Jensen & Claus Henrik Nielsen
Pages: 1203-1208
Published online: 21 Sep 2017
AbstractforReactive oxygen species inhibit catalytic activity of peptidylarginine deiminase | Full Text | References | PDF (736.5 KB) | Supplemental
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Article
Characterization of human S-adenosyl-homocysteine hydrolase in vitro and identification of its potential inhibitors
Weiwei Hao, Yanhua Li, Qiuli Shan, Tian Han, Wencheng Li, Sheng He, Kongkai Zhu, Yumei Li, Xiaojun Tan & Jinsong Gu
Pages: 1209-1215
Published online: 21 Sep 2017
AbstractforCharacterization of human S-adenosyl-homocysteine hydrolase in vitro and identification of its potential inhibitors | Full Text | References | PDF (1,023.3 KB)
  • 1531 Views
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Article
α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study
Carina Proença, Marisa Freitas, Daniela Ribeiro, Eduardo F. T. Oliveira, Joana L. C. Sousa, Sara M. Tomé, Maria J. Ramos, Artur M. S. Silva, Pedro A. Fernandes & Eduarda Fernandes
Pages: 1216-1228
Published online: 21 Sep 2017
Abstractforα-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study | Full Text | References | PDF (1.9 MB) | Supplemental
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Article
Synthesis, in vitro antitumour activity, and molecular docking study of novel 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinone analogues
Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Hazem A. Ghabbour & Manal A. Al-Gendy
Pages: 1229-1239
Published online: 26 Sep 2017
AbstractforSynthesis, in vitro antitumour activity, and molecular docking study of novel 2-substituted mercapto-3-(3,4,5-trimethoxybenzyl)-4(3H)-quinazolinone analogues | Full Text | References | PDF (1.3 MB) | Supplemental
  • 1366 Views
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Article
Development of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors
Carlotta Granchi, Isabella Caligiuri, Eleonora Bertelli, Giulio Poli, Flavio Rizzolio, Marco Macchia, Adriano Martinelli, Filippo Minutolo & Tiziano Tuccinardi
Pages: 1240-1252
Published online: 22 Sep 2017
AbstractforDevelopment of terphenyl-2-methyloxazol-5(4H)-one derivatives as selective reversible MAGL inhibitors | Full Text | References | PDF (1.9 MB)
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Article
Psychoactive substances belonging to the amphetamine class potently activate brain carbonic anhydrase isoforms VA, VB, VII, and XII
Andrea Angeli, Fabio Vaiano, Francesco Mari, Elisabetta Bertol & Claudiu T. Supuran
Pages: 1253-1259
Published online: 22 Sep 2017
AbstractforPsychoactive substances belonging to the amphetamine class potently activate brain carbonic anhydrase isoforms VA, VB, VII, and XII | Full Text | References | PDF (848.4 KB)
  • 1695 Views
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Article
Dual targeting of cancer-related human matrix metalloproteinases and carbonic anhydrases by chiral N-(biarylsulfonyl)-phosphonic acids
Grazia Luisi, Guido Angelini, Carla Gasbarri, Antonio Laghezza, Mariangela Agamennone, Fulvio Loiodice, Claudiu T. Supuran, Cristina Campestre & Paolo Tortorella
Pages: 1260-1264
Published online: 26 Sep 2017
AbstractforDual targeting of cancer-related human matrix metalloproteinases and carbonic anhydrases by chiral N-(biarylsulfonyl)-phosphonic acids | Full Text | References | PDF (717.7 KB)
  • 829 Views
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Article
Neem oil nanoemulsions: characterisation and antioxidant activity
Federica Rinaldi, Patrizia Nadia Hanieh, Catia Longhi, Simone Carradori, Daniela Secci, Gokhan Zengin, Maria Grazia Ammendolia, Elena Mattia, Elena Del Favero, Carlotta Marianecci & Maria Carafa
Pages: 1265-1273
Published online: 02 Oct 2017
AbstractforNeem oil nanoemulsions: characterisation and antioxidant activity | Full Text | References | PDF (1.3 MB)
  • 6059 Views
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Article
Discovery of curcumin inspired sulfonamide derivatives as a new class of carbonic anhydrase isoforms I, II, IX, and XII inhibitors
P. V. Sri Ramya, Srinivas Angapelly, Andrea Angeli, Chander Singh Digwal, Mohammed Arifuddin, Bathini Nagendra Babu, Claudiu T. Supuran & Ahmed Kamal
Pages: 1274-1281
Published online: 02 Oct 2017
AbstractforDiscovery of curcumin inspired sulfonamide derivatives as a new class of carbonic anhydrase isoforms I, II, IX, and XII inhibitors | Full Text | References | PDF (1.2 MB)
  • 1561 Views
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Short Communication

Rapid Communication
Resveratrol-based cinnamic ester hybrids: synthesis, characterization, and anti-inflammatory activity
Ban-Feng Ruan, Wei-Wei Ge, Hui-Jie Cheng, Hua-Jian Xu, Qing-Shan Li & Xin-Hua Liu
Pages: 1282-1290
Published online: 26 Oct 2017
AbstractforResveratrol-based cinnamic ester hybrids: synthesis, characterization, and anti-inflammatory activity | Full Text | References | PDF (2.3 MB) | Supplemental
  • 1489 Views
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Research Paper

Article
Antimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VII8–12
Anda-Mihaela Olaru, Violeta Vasilache, Ramona Danac & Ionel I. Mangalagiu
Pages: 1291-1298
Published online: 26 Oct 2017
AbstractforAntimycobacterial activity of nitrogen heterocycles derivatives: 7-(pyridine-4-yl)-indolizine derivatives. Part VII8–12 | Full Text | References | PDF (1,014 KB) | Supplemental
  • 1308 Views
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Article
In vitro and in vivo antitumour effects of phenylboronic acid against mouse mammary adenocarcinoma 4T1 and squamous carcinoma SCCVII cells
Maja Marasovic, Sinisa Ivankovic, Ranko Stojkovic, Damir Djermic, Borivoj Galic & Mladen Milos
Pages: 1299-1304
Published online: 26 Oct 2017
AbstractforIn vitro and in vivo antitumour effects of phenylboronic acid against mouse mammary adenocarcinoma 4T1 and squamous carcinoma SCCVII cells | Full Text | References | PDF (680.1 KB)
  • 1245 Views
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Article
Synthesis and biological evaluation of histamine Schiff bases as carbonic anhydrase I, II, IV, VII, and IX activators
Suleyman Akocak, Nabih Lolak, Daniela Vullo, Mustafa Durgun & Claudiu T. Supuran
Pages: 1305-1312
Published online: 26 Oct 2017
AbstractforSynthesis and biological evaluation of histamine Schiff bases as carbonic anhydrase I, II, IV, VII, and IX activators | Full Text | References | PDF (943.8 KB)
  • 1584 Views
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Editorial Board

Editorial Board
Page: ebi
Published online: 30 Oct 2017
CitationforEditorial Board | Full Text | PDF (28.8 KB)
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