Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 30, Issue 1 (2015)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 30, Issue 1 (2015)

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Original Article

Article
Novel phenolic inhibitors of the sarco/endoplasmic reticulum calcium ATPase: identification and characterization by quantitative structure–activity relationship modeling and virtual screening
Stefan Paula, Emily Hofmann, John Burden & David T. Stanton
Pages: 1-8
Published online: 11 Feb 2014
AbstractforNovel phenolic inhibitors of the sarco/endoplasmic reticulum calcium ATPase: identification and characterization by quantitative structure–activity relationship modeling and virtual screening | Full Text | References | PDF (425.1 KB) | Supplemental
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Original Articles

Article
Ginsenoside F2 possesses anti-obesity activity via binding with PPARγ and inhibiting adipocyte differentiation in the 3T3-L1 cell line
Fayeza Md. Siraj, Natarajan SathishKumar, Yeon Ju Kim, Se Young Kim & Deok Chun Yang
Pages: 9-14
Published online: 25 Mar 2014
AbstractforGinsenoside F2 possesses anti-obesity activity via binding with PPARγ and inhibiting adipocyte differentiation in the 3T3-L1 cell line | Full Text | References | PDF (1,000 KB)
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Research Article

Article
Potential pancreatic lipase inhibitory activity of an endophytic Penicillium species
Mahiti Gupta, Sanjai Saxena & Dinesh Goyal
Pages: 15-21
Published online: 14 Jan 2014
AbstractforPotential pancreatic lipase inhibitory activity of an endophytic Penicillium species | Full Text | References | PDF (686.4 KB)
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Article
Design, synthesis, characterization and in vitro and in vivo anti-inflammatory evaluation of novel pyrazole-based chalcones
Hemant V. Chavan, Laxman K. Adsul, Amol S. Kotmale, Valmik D. Dhakane, Vishnu N. Thakare & Babasaheb P. Bandgar
Pages: 22-31
Published online: 25 Mar 2014
AbstractforDesign, synthesis, characterization and in vitro and in vivo anti-inflammatory evaluation of novel pyrazole-based chalcones | Full Text | References | PDF (562.3 KB) | Supplemental
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Article
Synthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II)
Mehlika Dilek Altintop, Ahmet Ozdemir, Kaan Kucukoglu, Gulhan Turan-Zitouni, Hayrunnisa Nadaroglu & Zafer Asim Kaplancikli
Pages: 32-37
Published online: 25 Mar 2014
AbstractforSynthesis and evaluation of new thiadiazole derivatives as potential inhibitors of human carbonic anhydrase isozymes (hCA-I and hCA-II) | Full Text | References | PDF (275 KB)
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Article
Antioxidant, anti-inflammatory potential and chemical constituents of Origanum dubium Boiss., growing wild in Cyprus
Anastasia Karioti, Tanja Milošević-Ifantis, Nikitas Pachopos, Niki Niryiannaki, Dimitra Hadjipavlou-Litina & Helen Skaltsa
Pages: 38-43
Published online: 25 Mar 2014
AbstractforAntioxidant, anti-inflammatory potential and chemical constituents of Origanum dubium Boiss., growing wild in Cyprus | Full Text | References | PDF (202.8 KB)
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Article
New pyrano[2,3-c]pyridazine derivatives with antimicrobial activity synthesized using piperidine as the organocatalyst
Nadia G. Kandile & Howida T. Zaky
Pages: 44-51
Published online: 25 Mar 2014
AbstractforNew pyrano[2,3-c]pyridazine derivatives with antimicrobial activity synthesized using piperidine as the organocatalyst | Full Text | References | PDF (673.4 KB)
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Article
Inhibition of human carbonic anhydrase isozymes I, II, IX and XII with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl moieties
Ahmed M. Alafeefy, Hatem A. Abdel-Aziz, Daniela Vullo, Abdul-Malek S. Al-Tamimi, Amani S. Awaad, Menshawy A. Mohamed, Clemente Capasso & Claudiu T. Supuran
Pages: 52-56
Published online: 25 Mar 2014
AbstractforInhibition of human carbonic anhydrase isozymes I, II, IX and XII with a new series of sulfonamides incorporating aroylhydrazone-, [1,2,4]triazolo[3,4-b][1,3,4]thiadiazinyl- or 2-(cyanophenylmethylene)-1,3,4-thiadiazol-3(2H)-yl moieties | Full Text | References | PDF (185.6 KB)
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Original Article

Article
Transport mechanisms of a novel antileukemic and antiviral compound 9-norbornyl-6-chloropurine
Pavla Plačková, Hubert Hřebabecký, Michal Šála, Radim Nencka, Tomáš Elbert & Helena Mertlíková-Kaiserová
Pages: 57-62
Published online: 31 Mar 2014
AbstractforTransport mechanisms of a novel antileukemic and antiviral compound 9-norbornyl-6-chloropurine | Full Text | References | PDF (339.7 KB) | Supplemental
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Research Article

Article
Kinetic and structural characterization of an alternatively spliced variant of human mitochondrial 5′(3′)-deoxyribonucleotidase
Petr Pachl, Milan Fábry, Václav Veverka, Jiří Brynda & Pavlína Řezáčová
Pages: 63-68
Published online: 10 Feb 2014
AbstractforKinetic and structural characterization of an alternatively spliced variant of human mitochondrial 5′(3′)-deoxyribonucleotidase | Full Text | References | PDF (765.2 KB)
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Article
Purification of bovine serum paraoxonase and its immobilization on Eupergit C 250 L by covalent attachment
Murat Sayın & Ozen Ozensoy Guler
Pages: 69-74
Published online: 31 Mar 2014
AbstractforPurification of bovine serum paraoxonase and its immobilization on Eupergit C 250 L by covalent attachment | Full Text | References | PDF (433 KB)
  • 637 Views
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Article
Synthesis and biological activity of novel thiourea derivatives as carbonic anhydrase inhibitors
Neslihan Korkmaz, Oday A. Obaidi, Murat Senturk, Demet Astley, Deniz Ekinci & Claudiu T. Supuran
Pages: 75-80
Published online: 25 Mar 2014
AbstractforSynthesis and biological activity of novel thiourea derivatives as carbonic anhydrase inhibitors | Full Text | References | PDF (275 KB)
  • 2759 Views
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Article
Investigation of arenesulfonyl-2-imidazolidinones as potent carbonic anhydrase inhibitors
Alaa A-M. Abdel-Aziz, Adel S. El-Azab, Deniz Ekinci, Murat Şentürk & Claudiu T. Supuran
Pages: 81-84
Published online: 25 Mar 2014
AbstractforInvestigation of arenesulfonyl-2-imidazolidinones as potent carbonic anhydrase inhibitors | Full Text | References | PDF (164.4 KB)
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Original Article

Article
Design, synthesis and pharmacological evaluation of indolylsulfonamide amines as potent and selective 5-HT6 receptor antagonists
Ramakrishna V. S. Nirogi, Thrinath Reddy Bandyala, Veena Reballi, Jagadishu Babu Konda, Anand V. Daulatabad & Mukkanti Khagga
Pages: 85-97
Published online: 25 Mar 2014
AbstractforDesign, synthesis and pharmacological evaluation of indolylsulfonamide amines as potent and selective 5-HT6 receptor antagonists | Full Text | References | PDF (532.1 KB)
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Original Articles

Article
Discovery of butyrylcholinesterase inhibitors among derivatives of azaphenothiazines
Krzysztof Lodarski, Jakub Jończyk, Natalia Guzior, Marek Bajda, Joanna Gładysz, Joanna Walczyk, Małgorzata Jeleń, Beata Morak-Młodawska, Krystian Pluta & Barbara Malawska
Pages: 98-106
Published online: 25 Mar 2014
AbstractforDiscovery of butyrylcholinesterase inhibitors among derivatives of azaphenothiazines | Full Text | References | PDF (981.9 KB) | Supplemental
  • 1208 Views
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Research Article

Article
2-Chloro-1,4-naphthoquinone derivative of quercetin as an inhibitor of aldose reductase and anti-inflammatory agent
Ivana Milackova, Marta Soltesova Prnova, Magdalena Majekova, Ruzena Sotnikova, Michal Stasko, Lucia Kovacikova, Sreeparna Banerjee, Miroslav Veverka & Milan Stefek
Pages: 107-113
Published online: 25 Mar 2014
Abstractfor2-Chloro-1,4-naphthoquinone derivative of quercetin as an inhibitor of aldose reductase and anti-inflammatory agent | Full Text | References | PDF (480.5 KB)
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Article
Computational investigation of the selectivity of salen and tetrahydrosalen compounds towards the tumor-associated hCA XII isozyme
Atilla Akdemir, Celeste De Monte, Simone Carradori & Claudiu T. Supuran
Pages: 114-118
Published online: 25 Mar 2014
AbstractforComputational investigation of the selectivity of salen and tetrahydrosalen compounds towards the tumor-associated hCA XII isozyme | Full Text | References | PDF (597.8 KB)
  • 718 Views
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Original Article

Article
New barbiturates and thiobarbiturates as potential enzyme inhibitors
Ashfaq M Qureshi, Saira Mumtaz, Abdul Rauf, Muhammad Ashraf, Rumana Nasar & Zahid H Chohan
Pages: 119-125
Published online: 25 Mar 2014
AbstractforNew barbiturates and thiobarbiturates as potential enzyme inhibitors | Full Text | References | PDF (236.6 KB) | Supplemental
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Article
Design, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors
Andrii Anatoliyovych Gryshchenko, Kostiantyn Vasyliovych Levchenko, Volodymyr Grygorovich Bdzhola, Tatiana Panasivna Ruban, Lyubov Leonidovna Lukash & Sergiy Mikolayovych Yarmoluk
Pages: 126-132
Published online: 18 Jun 2014
AbstractforDesign, synthesis and biological evaluation of naphthostyril derivatives as novel protein kinase FGFR1 inhibitors | Full Text | References | PDF (456 KB)
  • 1272 Views
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Article
Cholinesterase inhibitory triterpenoids from the bark of Garcinia hombroniana
Nargis Jamila, Melati Khairuddean, Khaw Kooi Yeong, Hasnah Osman & Vikneswaran Murugaiyah
Pages: 133-139
Published online: 25 Mar 2014
AbstractforCholinesterase inhibitory triterpenoids from the bark of Garcinia hombroniana | Full Text | References | PDF (519.1 KB) | Supplemental
  • 1869 Views
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Article
Synthesis and in vitro biological evaluation of new heterocycles based on the indole moiety
Nadia G. Kandile, Mansoura I. Mohamed & Hind M. Ismaeel
Pages: 140-151
Published online: 31 Mar 2014
AbstractforSynthesis and in vitro biological evaluation of new heterocycles based on the indole moiety | Full Text | References | PDF (697.2 KB)
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Review Article

Recent advances in structure of progestins and their binding to progesterone receptors
Marisa Cabeza, Yvonne Heuze, Araceli Sánchez, Mariana Garrido & Eugene Bratoeff
Pages: 152-159
Published online: 25 Mar 2014
AbstractforRecent advances in structure of progestins and their binding to progesterone receptors | Full Text | References | PDF (871.1 KB)
  • 4131 Views
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Short Communication

Structure-based drug design and biological evaluation of 2-acetamidobenzothiazole derivative as EGFR kinase inhibitor
Moustafa T. Gabr, Nadia S. El-Gohary, Eman R. El-Bendary & Mohamed M. El-Kerdawy
Pages: 160-165
Published online: 07 Mar 2014
AbstractforStructure-based drug design and biological evaluation of 2-acetamidobenzothiazole derivative as EGFR kinase inhibitor | Full Text | References | PDF (672.4 KB) | Supplemental
  • 1023 Views
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Design, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors
Laura Friggeri, Daniela De Vita, Fabiana Pandolfi, Silvano Tortorella, Roberta Costi, Roberto Di Santo & Luigi Scipione
Pages: 166-172
Published online: 11 Feb 2014
AbstractforDesign, synthesis and evaluation of 3,4-dihydroxybenzoic acid derivatives as antioxidants, bio-metal chelating agents and acetylcholinesterase inhibitors | Full Text | References | PDF (534.8 KB) | Supplemental
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