Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue sup3 (2016)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue sup3 (2016)

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Research Article

Article
Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities
Emin Garibov, Parham Taslimi, Afsun Sujayev, Zeynebe Bingol, Songul Çetinkaya, İlhami Gulçin, Sukru Beydemir, Vagif Farzaliyev, Saleh H. Alwasel & Claudiu T. Supuran
Pages: 1-9
Published online: 22 Jun 2016
AbstractforSynthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities | Full Text | References | PDF (371.5 KB)
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Article
Synthesis and biological evaluation of 2-fluoro and 3-trifluoromethyl-phenyl-piperazinylalkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione as potential antidepressant agents
Agnieszka Zagórska, Adam Bucki, Marcin Kołaczkowski, Agata Siwek, Monika Głuch-Lutwin, Gabriela Starowicz, Grzegorz Kazek, Anna Partyka, Anna Wesołowska, Karolina Słoczyńska, Elżbieta Pękala & Maciej Pawłowski
Pages: 10-24
Published online: 29 Jun 2016
AbstractforSynthesis and biological evaluation of 2-fluoro and 3-trifluoromethyl-phenyl-piperazinylalkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione as potential antidepressant agents | Full Text | References | PDF (1.4 MB) | Supplemental
  • 1759 Views
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Article
Screening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light
Faten Alchab, Estelle Sibille, Laurent Ettouati, Emilie Bana, Zouhair Bouaziz, Angélique Mularoni, Elodie Monniot, Denyse Bagrel, Joachim Jose, Marc Le Borgne & Patrick Chaimbault
Pages: 25-32
Published online: 30 Jun 2016
AbstractforScreening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light | Full Text | References | PDF (607.7 KB)
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Article
An evolutionarily conserved allosteric site modulates beta-lactamase activity
Fatma Gizem Avci, Fatma Ece Altinisik, Didem Vardar Ulu, Elif Ozkirimli Olmez & Berna Sariyar Akbulut
Pages: 33-40
Published online: 28 Jun 2016
AbstractforAn evolutionarily conserved allosteric site modulates beta-lactamase activity | Full Text | References | PDF (642.1 KB)
  • 2238 Views
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Article
Synthesis and pharmacological evaluation of donepezil-based agents as new cholinesterase/monoamine oxidase inhibitors for the potential application against Alzheimer’s disease
Fan Li, Zhi-Min Wang, Jia-Jia Wu, Jin Wang, Sai-Sai Xie, Jin-Shuai Lan, Wei Xu, Ling-Yi Kong & Xiao-Bing Wang
Pages: 41-53
Published online: 07 Jul 2016
AbstractforSynthesis and pharmacological evaluation of donepezil-based agents as new cholinesterase/monoamine oxidase inhibitors for the potential application against Alzheimer’s disease | Full Text | References | PDF (1.4 MB) | Supplemental
  • 3210 Views
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Article
Synthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,5-diarylpyrazole derivatives
Khaled R. A. Abdellatif, Wael A. A. Fadaly, Waleed A. M. Ali & Gehan M. Kamel
Pages: 54-60
Published online: 10 Aug 2016
AbstractforSynthesis, cyclooxygenase inhibition, anti-inflammatory evaluation and ulcerogenic liability of new 1,5-diarylpyrazole derivatives | Full Text | References | PDF (426.2 KB)
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Article
Comparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid dehydrogenase type 1
Bianka Edina Herman, Johanna Szabó, Ildikó Bacsa, János Wölfling, Gyula Schneider, Mónika Bálint, Csaba Hetényi, Erzsébet Mernyák & Mihály Szécsi
Pages: 61-69
Published online: 18 Jul 2016
AbstractforComparative investigation of the in vitro inhibitory potencies of 13-epimeric estrones and D-secoestrones towards 17β-hydroxysteroid dehydrogenase type 1 | Full Text | References | PDF (723.9 KB) | Supplemental
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Article
Impact of calcium ion on cytotoxic effect of the boroxine derivative, K2[B3O3F4OH]
Sinisa Ivankovic, Ranko Stojkovic, Milka Maksimovic, Borivoj Galic & Mladen Milos
Pages: 70-74
Published online: 07 Jul 2016
AbstractforImpact of calcium ion on cytotoxic effect of the boroxine derivative, K2[B3O3F4OH] | Full Text | References | PDF (261.7 KB)
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Article
P/CAF-mediated spermidine acetylation regulates histone acetyltransferase activity
Giosalba Burgio, Davide F. V. Corona, Concetta M. A. Nicotra, Giuseppe Carruba & Gennaro Taibi
Pages: 75-82
Published online: 07 Jul 2016
AbstractforP/CAF-mediated spermidine acetylation regulates histone acetyltransferase activity | Full Text | References | PDF (1.2 MB)
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Article
Synthesis and biological evaluation of novel propargylquinobenzothiazines and their derivatives as potential antiproliferative, anti-inflammatory, and anticancer agents
Małgorzata Jeleń, Krystian Pluta, Michał Zimecki, Beata Morak-Młodawska, Jolanta Artym, Maja Kocięba & Iwona Kochanowska
Pages: 83-88
Published online: 12 Jul 2016
AbstractforSynthesis and biological evaluation of novel propargylquinobenzothiazines and their derivatives as potential antiproliferative, anti-inflammatory, and anticancer agents | Full Text | References | PDF (201.6 KB) | Supplemental
  • 1105 Views
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Article
Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities
Yasemin Ünver, Sadik Deniz, Fatih Çelik, Zeynep Akar, Murat Küçük & Kemal Sancak
Pages: 89-95
Published online: 18 Jul 2016
AbstractforSynthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities | Full Text | References | PDF (333.9 KB) | Supplemental
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Article
A comparative study of the antihyaluronidase, antiurease, antioxidant, antimicrobial and physicochemical properties of different unifloral degrees of chestnut (Castanea sativa Mill.) honeys
Sevgi Kolayli, Zehra Can, Oktay Yildiz, Huseyin Sahin & Sengul Alpay Karaoglu
Pages: 96-104
Published online: 20 Jul 2016
AbstractforA comparative study of the antihyaluronidase, antiurease, antioxidant, antimicrobial and physicochemical properties of different unifloral degrees of chestnut (Castanea sativa Mill.) honeys | Full Text | References | PDF (262.1 KB)
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Article
Synthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones
Elif Unluer, Halise Inci Gul, Alkan Demirtas, Hiroshi Sakagami, Naoki Umemura, Muhammet Tanc, Cavit Kazaz & Claudiu T. Supuran
Pages: 105-109
Published online: 19 Jul 2016
AbstractforSynthesis and bioactivity studies of 1-aryl-3-(2-hydroxyethylthio)-1-propanones | Full Text | References | PDF (225.9 KB)
  • 767 Views
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Article
Microextraction by packed sorbent and HPLC–PDA quantification of multiple anti-inflammatory drugs and fluoroquinolones in human plasma and urine
Veronica D’Angelo, Francesco Tessari, Giuseppe Bellagamba, Elisa De Luca, Roberta Cifelli, Christian Celia, Rosita Primavera, Martina Di Francesco, Donatella Paolino, Luisa Di Marzio & Marcello Locatelli
Pages: 110-116
Published online: 22 Jul 2016
AbstractforMicroextraction by packed sorbent and HPLC–PDA quantification of multiple anti-inflammatory drugs and fluoroquinolones in human plasma and urine | Full Text | References | PDF (460.8 KB) | Supplemental
  • 1526 Views
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Article
Development of the β-lactam type molecular scaffold for selective estrogen receptor α modulator action: synthesis and cytotoxic effects in MCF-7 breast cancer cells
Miriam Carr, Andrew J. S. Knox, David G. Lloyd, Daniela M. Zisterer & Mary J. Meegan
Pages: 117-130
Published online: 01 Aug 2016
AbstractforDevelopment of the β-lactam type molecular scaffold for selective estrogen receptor α modulator action: synthesis and cytotoxic effects in MCF-7 breast cancer cells | Full Text | References | PDF (1.3 MB) | Supplemental
  • 985 Views
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Article
Kinetic and computational analysis of the reversible inhibition of porcine pancreatic elastase: a structural and mechanistic approach
Panagiota-Yiolanda Stergiou, Athanasios Foukis, Olga A. Gkini, Joseph G. Bieth & Emmanuel M. Papamichael
Pages: 131-139
Published online: 04 Aug 2016
AbstractforKinetic and computational analysis of the reversible inhibition of porcine pancreatic elastase: a structural and mechanistic approach | Full Text | References | PDF (1.9 MB) | Supplemental
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Original Article

Article
N-(2-hydroxyphenyl)-2-propylpentanamide, a valproic acid aryl derivative designed in silico with improved anti-proliferative activity in HeLa, rhabdomyosarcoma and breast cancer cells
Berenice Prestegui-Martel, Jorge Antonio Bermúdez-Lugo, Alma Chávez-Blanco, Alfonso Dueñas-González, José Rubén García-Sánchez, Oscar Alberto Pérez-González, Itzia Irene Padilla-Martínez, Manuel Jonathan Fragoso-Vázquez, Jessica Elena Mendieta-Wejebe, Ana María Correa-Basurto, David Méndez-Luna, José Trujillo-Ferrara & José Correa-Basurto
Pages: 140-149
Published online: 02 Aug 2016
AbstractforN-(2-hydroxyphenyl)-2-propylpentanamide, a valproic acid aryl derivative designed in silico with improved anti-proliferative activity in HeLa, rhabdomyosarcoma and breast cancer cells | Full Text | References | PDF (1 MB)
  • 2789 Views
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Article
Biological evaluation of dimethylpyridine–platinum complexes with potent antiproliferative activity
Robert Czarnomysy, Krzysztof Bielawski, Anna Muszynska, Anna Bielawska & Agnieszka Gornowicz
Pages: 150-165
Published online: 04 Aug 2016
AbstractforBiological evaluation of dimethylpyridine–platinum complexes with potent antiproliferative activity | Full Text | References | PDF (3.6 MB)
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Research Article

Article
Synthesis and antiproliferative activity of some N′-substituted 2,4-dihydroxybenzothiohydrazides
Joanna Matysiak, Alicja Skrzypek, Monika Karpińska, Urszula Głaszcz, Andrzej Niewiadomy, Beata Paw, Bogusław Senczyna, Joanna Wietrzyk & Dagmara Kłopotowska
Pages: 166-172
Published online: 26 Jul 2016
AbstractforSynthesis and antiproliferative activity of some N′-substituted 2,4-dihydroxybenzothiohydrazides | Full Text | References | PDF (402.7 KB)
  • 777 Views
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Article
Synthesis, characterization and in vitro evaluation of substituted N-(2-phenylcyclopropyl)carbamates as acetyl- and butyrylcholinesterase inhibitors
Eva Horáková, Pavel Drabina, Břetislav Brož, Šárka Štěpánková, Katarína Vorčáková, Karel Královec, Radim Havelek & Miloš Sedlák
Pages: 173-179
Published online: 01 Aug 2016
AbstractforSynthesis, characterization and in vitro evaluation of substituted N-(2-phenylcyclopropyl)carbamates as acetyl- and butyrylcholinesterase inhibitors | Full Text | References | PDF (299.1 KB) | Supplemental
  • 1535 Views
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Review Article

Review
Cholinesterase-based biosensors
Šárka Štěpánková & Katarína Vorčáková
Pages: 180-193
Published online: 12 Jul 2016
AbstractforCholinesterase-based biosensors | Full Text | References | PDF (443.8 KB)
  • 4644 Views
  • 28 CrossRef citations
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Research Article

Review
The role of modulation of antioxidant enzyme systems in the treatment of neurodegenerative diseases
Sybil Obuobi, Sanzhar Karatayev, Christina Li Lin Chai, Pui Lai Rachel Ee & Peter Mátyus
Pages: 194-204
Published online: 07 Jul 2016
AbstractforThe role of modulation of antioxidant enzyme systems in the treatment of neurodegenerative diseases | Full Text | References | PDF (902.5 KB)
  • 1956 Views
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Short Communication

Rapid Communication
Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase
Shima Dianat, Setareh Moghimi, Mohammad Mahdavi, Hamid Nadri, Alireza Moradi, Loghman Firoozpour, Saeed Emami, Arash Mouradzadegun, Abbas Shafiee & Alireza Foroumadi
Pages: 205-209
Published online: 17 Jul 2016
AbstractforQuinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase | Full Text | References | PDF (654.5 KB) | Supplemental
  • 1672 Views
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