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首页> 外文期刊>Indian Journal of Heterocyclic Chemistry. (Text in English) >SYNTHESIS OF NOVEL SERIES OF SUBSTITUTED 1,3,4-THIADIAZOLE/IMIDAZO (2,1-b)-1,3,4-THIADIAZOLES; A NOVEL CLASS OF POTENT ANTIINFLAMMATORY AND ANALGESIC AGENTS
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SYNTHESIS OF NOVEL SERIES OF SUBSTITUTED 1,3,4-THIADIAZOLE/IMIDAZO (2,1-b)-1,3,4-THIADIAZOLES; A NOVEL CLASS OF POTENT ANTIINFLAMMATORY AND ANALGESIC AGENTS

机译:取代的1,3,4-噻二唑/咪唑(2,1-b)-1,3,4-噻二唑新系列化合物的合成;新型强效抗炎和止痛剂

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摘要

A novel series of substituted 1,3,4-thiadiazoles (3a-b) and imidazo (2,1-b)-1,3,4-thiadiazoles (4a-j) were synthesized by the reaction between Schiff bases of 1,3,4-thiadiazoles (2a-b) with thioglycollic acid in the presence of ethanol and 2-amino-5-(substituted phenyl)-1,3,4-thiadiazoles (1a-c) with different substituted aryl/heteroaryl α-bromoketones in dry ethanol respectively. The purity of these compounds was confirmed by melting point and TLC. Structures of these compounds were confirmed on the basis of IR, ~1H NMR and Mass spectral data. The title compounds were screened for antiinflammatory and analgesic activities using carrageenan induced rat paw edema method and acetic acid induced writhing method respectively. The results showed that compounds 4b, 4c, 4d, 4i and 4j exhibited good anti-inflammatory activity as compared with standard drug Diclofenac and compounds 4b, 4c and 4i showed good analgesic activity as compared with standard drug Aspirin.
机译:通过1的席夫碱之间的反应合成了一系列新的取代的1,3,4-噻二唑(3a-b)和咪唑(2,1-b)-1,3,4-噻二唑(4a-j)。 3,4-噻二唑(2a-b)与巯基乙酸在乙醇存在下和2-氨基-5-(取代的苯基)-1,3,4-噻二唑(1a-c)与不同的取代芳基/杂芳基α-分别在无水乙醇中的溴代酮。这些化合物的纯度通过熔点和TLC确认。这些化合物的结构根据IR,〜1H NMR和质谱数据确定。分别使用角叉菜胶诱导的大鼠爪水肿法和乙酸诱导的扭体法筛选标题化合物的抗炎和镇痛活性。结果表明,与标准药物双氯芬酸相比,化合物4b,4c,4d,4i和4j显示出良好的抗炎活性,与标准药物阿司匹林相比,化合物4b,4c和4i显示出良好的镇痛活性。

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