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新型 5-取代-1-(苯磺酰基)-2-甲基苯并咪唑衍生物的合成及抗炎镇痛活性评价。

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

机构信息

Department of Pharmaceutical Sciences, ASBASJSM College of Pharmacy, Bela, Ropar, Punjab, India.

出版信息

Eur J Med Chem. 2010 Jun;45(6):2245-9. doi: 10.1016/j.ejmech.2010.01.067. Epub 2010 Feb 2.

Abstract

A series of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives have been synthesized. The structures of these compounds were established by IR, 1H NMR, 13C 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.

摘要

已经合成了一系列新型的 5-取代-1-(苯磺酰基)-2-甲基苯并咪唑衍生物。这些化合物的结构通过红外光谱、1H NMR、13C NMR、质谱数据和元素分析确定。对这些化合物的抗炎和镇痛活性以及胃溃疡形成作用进行了评价。在角叉菜胶诱导的大鼠足肿胀和醋酸诱导的小鼠扭体反应中,衍生物 4a、4b 和 4c 分别表现出中等至良好的抗炎和镇痛活性,与标准药物吲哚美辛相比,溃疡形成作用较低。

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