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某些中氮茚并苯乙烯基酮作为潜在非甾体抗炎药的设计与合成

Design and synthesis of certain mesoionic sydnonyl styrylketones as potential nonsteroidal antiinflammatory agents.

作者信息

Deshpande Shreenivas Ramachandrarao, Pai Karkala Vasantakumar, Pai Ranganath Sridhar

机构信息

Department of Medicinal & Pharmaceutical Chemistry, HSK College of Pharmacy, BWS Campus, Bagalkote, Karnataka, India.

出版信息

Arzneimittelforschung. 2011;61(3):180-5. doi: 10.1055/s-0031-1296186.

DOI:10.1055/s-0031-1296186
PMID:21528643
Abstract

In an attempt to develop effective and safer analgesic anti-inflammatory agents, nine compounds belonging to 4-[1-oxo-3-(substituted aryl)-2-propenyl]-3-(4-methoxyphenyl) sydnones, containing the structural features of mesoionic sydnone and styrylketone, have been designed and synthesized by condensing 4-acetyl-3-(4-methoxyphenyl) sydnone with various substituted aryl aldehydes and characterized by spectral studies. They have been tested for analgesic activity by acetic acid induced writhing in mice and for anti-inflammatory activity by carrageenan induced rat paw edema at 100 mg/kg body weight p.o. The compounds containing furyl and chloro substituents showed highly significant analgesic effect, while those with dimethylamino, chloro and nitro substituents exhibited highly significant anti-inflammatory effect at the end of 3 h. The compounds that showed good analgesic and anti-inflammatory activities were evaluated for ulcerogenicity in rats to assess their gastric side effects at 100 mg/kg body weight p.o. They were found to be less ulcerogenic than the standard drug.

摘要

为了开发有效且更安全的镇痛抗炎药,设计并合成了九种属于4-[1-氧代-3-(取代芳基)-2-丙烯基]-3-(4-甲氧基苯基)斯德酮的化合物,这些化合物含有中氮茚酮和苯乙烯基酮的结构特征,通过将4-乙酰基-3-(4-甲氧基苯基)斯德酮与各种取代芳基醛缩合而成,并通过光谱研究进行了表征。通过乙酸诱导小鼠扭体试验测试了它们的镇痛活性,通过角叉菜胶诱导大鼠足爪肿胀试验在口服100mg/kg体重时测试了它们的抗炎活性。含有呋喃基和氯取代基的化合物显示出高度显著的镇痛效果,而含有二甲氨基、氯和硝基取代基的化合物在3小时末表现出高度显著的抗炎效果。对显示出良好镇痛和抗炎活性的化合物在大鼠中进行了致溃疡作用评估,以评估其在口服100mg/kg体重时的胃部副作用。发现它们的致溃疡作用比标准药物小。

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