1-(4-Methane(amino)sulfonylphenyl)-3-(4-substituted-phenyl)-5-(4-trifluoromethylphenyl)-1H-2-pyrazolines/pyrazoles as potential anti-inflammatory agents

被引：34

作者：

Abdellatif, Khaled R. A. ^{[1
]}

Elshemy, Heba A. H. ^{[1
]}

Azoz, Amany A. ^{[2
]}

机构：

[1] Beni Suef Univ, Dept Organ Pharmaceut Chem, Fac Pharm, Bani Suwayf 62514, Egypt

[2] Beni Suef Univ, Dept Pharmacol, Fac Pharm, Bani Suwayf 62514, Egypt

来源：

BIOORGANIC CHEMISTRY | 2015年 / 63卷

关键词：

Celecoxib analogs; Pyrazoline; Pyrazole; Cyclooxygenase-2; Anti-inflammatory activity; DONOR ESTER PRODRUGS; BIOLOGICAL EVALUATION; ANALOG SYNTHESIS; DERIVATIVES; CELECOXIB; ENZYMES; DESIGN;

D O I：

10.1016/j.bioorg.2015.09.002

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

070307 [化学生物学]; 071010 [生物化学与分子生物学];

摘要：

2-Pyrazolins 14a-l and pyrazoles 15a-l were designed as celecoxib analogs for the evaluation of their in vitro COX-1/COX-2 inhibitory activity and the in vivo anti-inflammatory activity. Compounds 14i, 15a, 15d and 15f were the most COX-2 selective derivatives (S.I. = 5.93, 6.08, 5.03 and 5.27 respectively) while the pyrazoline derivatives 14g and 14i exhibited the highest AI activity (ED50 = 190.5 and 160.1 mu mol/kg po, respectively). (C) 2015 Elsevier Inc. All rights reserved.

引用

页码：13 / 23

页数：11

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