Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue sup1 (2016)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 31, Issue sup1 (2016)

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Research Article

Article
Synthesis and biological evaluation of novel N1-phenylsulphonyl indole derivatives as potent and selective 5-HT6R ligands for the treatment of cognitive disorders
Ramakrishna V. S. Nirogi, Thrinath Reddy Bandyala, Pamuletinarasimha Reddy Gangadasari & Mukkanti Khagga
Pages: 1-15
Published online: 03 Nov 2016
AbstractforSynthesis and biological evaluation of novel N1-phenylsulphonyl indole derivatives as potent and selective 5-HT6R ligands for the treatment of cognitive disorders | Full Text | References | PDF (623.8 KB)
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Article
Human neutrophil elastase inhibitory potential of flavonoids from Campylotropis hirtella and their kinetics
Xue Fei Tan, Dae Wook Kim, Yeong Hun Song, Jeong Yoon Kim, Heung Joo Yuk, Yan Wang, Marcus J. Curtis-Long & Ki Hun Park
Pages: 16-22
Published online: 25 Aug 2016
AbstractforHuman neutrophil elastase inhibitory potential of flavonoids from Campylotropis hirtella and their kinetics | Full Text | References | PDF (841.3 KB) | Supplemental
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Article
Synthesis, cytotoxic, anti-lipoxygenase and anti-acetylcholinesterase capacities of novel derivatives from harmine
Insaf Filali, Mohamed Amine Belkacem, Aymen Ben Nejma, Jean Pierre Souchard, Hichem Ben Jannet & Jalloul Bouajila
Pages: 23-33
Published online: 30 Mar 2016
AbstractforSynthesis, cytotoxic, anti-lipoxygenase and anti-acetylcholinesterase capacities of novel derivatives from harmine | Full Text | References | PDF (405.1 KB)
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Original Article

Article
Synthesis and biological evaluation of novel 2-phenylquinazoline-4-amine derivatives: identification of 6-phenyl-8H-benzo[g]quinazolino[4,3-b]quinazolin-8-one as a highly potent inducer of NAD(P)H quinone oxidoreductase 1
Mostafa M. Ghorab, Mansour S. Alsaid, Marwa G. El-Gazzar, Maureen Higgins, Albena T. Dinkova-Kostova & Abdelaaty A. Shahat
Pages: 34-39
Published online: 01 Apr 2016
AbstractforSynthesis and biological evaluation of novel 2-phenylquinazoline-4-amine derivatives: identification of 6-phenyl-8H-benzo[g]quinazolino[4,3-b]quinazolin-8-one as a highly potent inducer of NAD(P)H quinone oxidoreductase 1 | Full Text | References | PDF (649.5 KB)
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Research Article

Article
Synthesis and structural analysis of halogen substituted fibril formation inhibitors of Human Transthyretin (TTR)
Lidia Ciccone, Susanna Nencetti, Armando Rossello, Enrico Adriano Stura & Elisabetta Orlandini
Pages: 40-51
Published online: 11 Apr 2016
AbstractforSynthesis and structural analysis of halogen substituted fibril formation inhibitors of Human Transthyretin (TTR) | Full Text | References | PDF (2.2 MB)
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Article
Inhibition properties of propolis extracts to some clinically important enzymes
Nimet Baltas, Oktay Yildiz & Sevgi Kolayli
Pages: 52-55
Published online: 07 Apr 2016
AbstractforInhibition properties of propolis extracts to some clinically important enzymes | Full Text | References | PDF (162.8 KB)
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Article
Protective effect of Naringin on experimental hindlimb ischemia/reperfusion injury in rats
Cebrail Gürsul, Fazile Nur Ekinci Akdemir, Turan Akkoyun, İsmail Can, Mustafa Gül & İlhami Gülçin
Pages: 56-61
Published online: 07 Apr 2016
AbstractforProtective effect of Naringin on experimental hindlimb ischemia/reperfusion injury in rats | Full Text | References | PDF (282.4 KB)
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Article
Hydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp
Łukasz Popiołek & Anna Biernasiuk
Pages: 62-69
Published online: 13 Apr 2016
AbstractforHydrazide-hydrazones of 3-methoxybenzoic acid and 4-tert-butylbenzoic acid with promising antibacterial activity against Bacillus spp | Full Text | References | PDF (257.2 KB)
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Article
Insights into the mechanism of inhibition of tryptophan 2,3-dioxygenase by isatin derivatives
Georgios Pantouris, James Loudon-Griffiths & Christopher G. Mowat
Pages: 70-78
Published online: 20 Apr 2016
AbstractforInsights into the mechanism of inhibition of tryptophan 2,3-dioxygenase by isatin derivatives | Full Text | References | PDF (1.7 MB) | Supplemental
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Article
The synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles
Burhanettin Turan, Kivilcim Şendil, Emin Şengül, Mehmet Serdar Gültekin, Parham Taslimi, İlhami Gulçin & Claudiu T. Supuran
Pages: 79-88
Published online: 13 Apr 2016
AbstractforThe synthesis of some β-lactams and investigation of their metal-chelating activity, carbonic anhydrase and acetylcholinesterase inhibition profiles | Full Text | References | PDF (627.2 KB) | Supplemental
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Article
Changing the selectivity profile – from substrate analog inhibitors of thrombin and factor Xa to potent matriptase inhibitors
Alexander Maiwald, Maya Hammami, Sebastian Wagner, Andreas Heine, Gerhard Klebe & Torsten Steinmetzer
Pages: 89-97
Published online: 11 May 2016
AbstractforChanging the selectivity profile – from substrate analog inhibitors of thrombin and factor Xa to potent matriptase inhibitors | Full Text | References | PDF (923.6 KB) | Supplemental
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Article
Targeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors
Margherita Brindisi, Simone Brogi, Simone Giovani, Sandra Gemma, Stefania Lamponi, Filomena De Luca, Ettore Novellino, Giuseppe Campiani, Jean-Denis Docquier & Stefania Butini
Pages: 98-109
Published online: 28 Apr 2016
AbstractforTargeting clinically-relevant metallo-β-lactamases: from high-throughput docking to broad-spectrum inhibitors | Full Text | References | PDF (1.1 MB)
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Article
Encapsulation of anti-carbonic anhydrase IX antibody in hydrogel microspheres for tumor targeting
Martina Takacova, Gabriela Hlouskova, Miriam Zatovicova, Martin Benej, Olga Sedlakova, Juraj Kopacek, Jaromir Pastorek, Igor Lacik & Silvia Pastorekova
Pages: 110-118
Published online: 03 May 2016
AbstractforEncapsulation of anti-carbonic anhydrase IX antibody in hydrogel microspheres for tumor targeting | Full Text | References | PDF (1.7 MB) | Supplemental
  • 1440 Views
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Article
Lansoprazole and carbonic anhydrase IX inhibitors sinergize against human melanoma cells
Cristina Federici, Luana Lugini, Maria Lucia Marino, Fabrizio Carta, Elisabetta Iessi, Tommaso Azzarito, Claudiu T. Supuran & Stefano Fais
Pages: 119-125
Published online: 03 May 2016
AbstractforLansoprazole and carbonic anhydrase IX inhibitors sinergize against human melanoma cells | Full Text | References | PDF (416.4 KB)
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Original Article

Article
Pyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity
Shaojuan Zhu, Shuzhen Zhang, Xin Hao, Xiangyu Qin, Shagufta Parveen, Shaoqi Yang, Bing Ma & Changjin Zhu
Pages: 126-130
Published online: 06 May 2016
AbstractforPyridothiadiazine derivatives as aldose reductase inhibitors having antioxidant activity | Full Text | References | PDF (1,008.8 KB) | Supplemental
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Research Article

Article
1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: bioisosteric replacement of the carboxylic acid moiety
Jan Althaus, Theresa Hake, Walburga Hanekamp & Matthias Lehr
Pages: 131-140
Published online: 09 May 2016
Abstractfor1-(5-Carboxyindazol-1-yl)propan-2-ones as dual inhibitors of cytosolic phospholipase A2α and fatty acid amide hydrolase: bioisosteric replacement of the carboxylic acid moiety | Full Text | References | PDF (507.8 KB) | Supplemental
  • 971 Views
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Article
Investigation of inhibition of human glucose 6-phosphate dehydrogenase by some 99mTc chelators by in silico and in vitro methods
Ali Şahin, Murat Şentürk, Ramin E. Salmas, Serdar Durdagi, Arif Ayan, Ali Karagölge & Mert Mestanoğlu
Pages: 141-147
Published online: 03 May 2016
AbstractforInvestigation of inhibition of human glucose 6-phosphate dehydrogenase by some 99mTc chelators by in silico and in vitro methods | Full Text | References | PDF (1.7 MB)
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Article
Effect of monohydroxylated flavonoids on glycation-induced lens opacity and protein aggregation
Kapil K. Patil, Rohan J. Meshram & Rajesh N. Gacche
Pages: 148-156
Published online: 05 May 2016
AbstractforEffect of monohydroxylated flavonoids on glycation-induced lens opacity and protein aggregation | Full Text | References | PDF (1.5 MB)
  • 1055 Views
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Article
Synthesis and biological evaluation of fluoropyrazolesulfonylurea and thiourea derivatives as possible antidiabetic agents
Hassan M. Faidallah, Manal M. Al-Mohammadi, Khalid A. Alamry & Khalid A. Khan
Pages: 157-163
Published online: 04 May 2016
AbstractforSynthesis and biological evaluation of fluoropyrazolesulfonylurea and thiourea derivatives as possible antidiabetic agents | Full Text | References | PDF (235.2 KB) | Supplemental
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Review Article

Review
[60]Fullerene-peptides: bio-nano conjugates with structural and chemical diversity
Andrew R. Barron
Pages: 164-176
Published online: 10 May 2016
Abstractfor[60]Fullerene-peptides: bio-nano conjugates with structural and chemical diversity | Full Text | References | PDF (2.3 MB)
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Review
Matrix metalloproteinases (MMPs), the main extracellular matrix (ECM) enzymes in collagen degradation, as a target for anticancer drugs
Agata Jabłońska-Trypuć, Marzena Matejczyk & Stanisław Rosochacki
Pages: 177-183
Published online: 30 Mar 2016
AbstractforMatrix metalloproteinases (MMPs), the main extracellular matrix (ECM) enzymes in collagen degradation, as a target for anticancer drugs | Full Text | References | PDF (361.4 KB)
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Review
Chinese herb medicine against Sortase A catalyzed transformations, a key role in gram-positive bacterial infection progress
Lifang Si, Pan Li, Xiong Liu & Lixin Luo
Pages: 184-196
Published online: 10 May 2016
AbstractforChinese herb medicine against Sortase A catalyzed transformations, a key role in gram-positive bacterial infection progress | Full Text | References | PDF (1.4 MB)
  • 2053 Views
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Short Communication

Rapid Communication
Isoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases
Claudiu T. Supuran, Stanislav Kalinin, Muhammet Tanç, Pakornwit Sarnpitak, Prashant Mujumdar, Sally-Ann Poulsen & Mikhail Krasavin
Pages: 197-202
Published online: 10 May 2016
AbstractforIsoform-selective inhibitory profile of 2-imidazoline-substituted benzene sulfonamides against a panel of human carbonic anhydrases | Full Text | References | PDF (320.8 KB) | Supplemental
  • 1307 Views
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Rapid Communication
Comparative study of biological activities and multicomponent pattern of two wild Turkish species: Asphodeline anatolica and Potentilla speciosa
Gokhan Zengin, Luigi Menghini, Luciano Malatesta, Elisa De Luca, Giuseppe Bellagamba, Sengul Uysal, Abdurrahman Aktumsek & Marcello Locatelli
Pages: 203-208
Published online: 03 May 2016
AbstractforComparative study of biological activities and multicomponent pattern of two wild Turkish species: Asphodeline anatolica and Potentilla speciosa | Full Text | References | PDF (258.8 KB) | Supplemental
  • 1641 Views
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Rapid Communication
Cell-based multi-substrate assay coupled to UHPLC-ESI-MS/MS for a quick identification of class-specific HDAC inhibitors
Vincent Zwick, Claudia Simões-Pires & Muriel Cuendet
Pages: 209-214
Published online: 05 May 2016
AbstractforCell-based multi-substrate assay coupled to UHPLC-ESI-MS/MS for a quick identification of class-specific HDAC inhibitors | Full Text | References | PDF (761.4 KB) | Supplemental
  • 1223 Views
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