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抗结核药物,I:2-芳基-1,3,4-噻二唑衍生物的合成与抗结核活性

Antituberculosis agents, I: Synthesis and antituberculosis activity of 2-aryl-1,3,4-thiadiazole derivatives.

作者信息

Foroumadi A, Mirzaei M, Shafiee A

机构信息

Research Center of Kerman University of Medical Sciences, Kerman, Iran.

出版信息

Pharmazie. 2001 Aug;56(8):610-2.

PMID:11534334
Abstract

The design, synthesis and antituberculosis activity of a series of 2-aryl-5-methylthio-1,3,4-thiadiazoles (5a-b), ethyl alpha-(5-aryl)-1,3,4-thiadiazole-2-ylthio)acetates (8a-b) and related compounds are described. All of the compounds were tested against Mycobacterium tuberculosis strain H37Rv in comparison to rifampicin. Six compounds exhibited a very good activity (MIC < 6.25 micrograms/ml, % Inhibition = 100).

摘要

描述了一系列2-芳基-5-甲硫基-1,3,4-噻二唑(5a-b)、α-(5-芳基)-1,3,4-噻二唑-2-基硫代乙酸乙酯(8a-b)及相关化合物的设计、合成与抗结核活性。所有化合物均与利福平相比,针对结核分枝杆菌H37Rv菌株进行了测试。六种化合物表现出非常好的活性(最低抑菌浓度<6.25微克/毫升,抑制率=100%)。

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