Pyrazolone Derivatives: Synthesis, Anti-inflammatory, Analgesic, Quantitative Structure-Activity Relationship and in Vitro Studies

被引：23

作者：

Ragab, Fatma Abdel-Fattah ^{[1
]}

Abdel-Gawad, Nagwa Mohamed ^{[1
]}

Georgey, Hanan Hanna ^{[1
]}

Said, Mona Fikry ^{[1
]}

机构：

[1] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11562, Egypt

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2013年 / 61卷 / 08期

关键词：

pyrazolone; acetic acid; quantitative structure-activity relationship; cyclooxygenase inhibition; anti-inflammatory; BIOLOGICAL EVALUATION; MYCOBACTERIUM-TUBERCULOSIS; SELECTIVE-INHIBITION; DRUGS; CYCLOOXYGENASE; ANALOGS; SERIES; AGENTS; QSAR; RAT;

D O I：

10.1248/cpb.c13-00314

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Some 1-(4-chlorophenyl or benzenesulfonamide)-2,3- and/or 4-substituted-1H-pyrazol-5(4H)-one derivatives were synthesized and screened for their anti-inflammatory and analgesic activities, in addition to their ulcerogenic liability. They were found to be active as anti-inflammatory and analgesic agents. Compound 6b was found to be the most active as anti-inflammatory agent and compound 9b was found to be the most active one as anti-inflammatory and analgesic agent. On the other hand, cyclooxygenase-1/-2 (COX-1)/COX-2 isozyme selectivity was also done and the tested compounds showed equal inhibition to both isoforms. Moreover, 2D-quantitative structure-activity relationship (QSAR) studies revealed well predictive and statistically significant and cross validated QSAR model that helps to explore some expectedly potent compounds.

引用

页码：834 / 845

页数：12

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