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

被引：22
|
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
收藏
页码：834 / 845
页数：12
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