Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents

被引：110

作者：

Gaba, Monika ^{[1
,2
]}

Singh, Dhandeep ^{[2
]}

Singh, Sarbjot ^{[2
,3
]}

Sharma, Vikas ^{[2
]}

Gaba, Punam ^{[1
]}

机构：

[1] ASBASJSM Coll Pharm, Dept Pharmaceut Chem, Bela, Ropar Punjab, India

[2] Punjabi Univ, Dept Pharmaceut Sci & Drug Res, Patiala, Punjab, India

[3] Panacea Biotech Pvt Ltd, Drug Discovery Res, Biol Res, Mohali, Punjab, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 06期

关键词：

2-Methylbenzimidazole; Analgesic activity; Anti-inflammatory activity; Carrageenan-induced paw edema model; SELECTIVE CYCLOOXYGENASE-2 INHIBITORS; 2-(5-ETHYLPYRIDIN-2-YL)BENZIMIDAZOLE KB-1043; GASTROINTESTINAL TOXICITY; AMIDE DERIVATIVES; ACETIC-ACID; DRUGS; POTENT; NSAIDS; ESTER;

D O I：

10.1016/j.ejmech.2010.01.067

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives have been synthesized. The structures of these compounds were established by IR, (1)H NMR, (13)C NMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activity as well as gastric ulcerogenic effects. Derivatives 4a, 4b and 4c exhibited moderate to good anti-inflammatory and analgesic activity in carrageenan-induced rat paw edema and acetic acid-induced writhing in mice, respectively, with low ulcerogenicity compared with the standard drug indomethacin.

引用

页码：2245 / 2249

页数：5