Antituberculosis agents. V. Synthesis, evaluation of in vitro antituberculosis activity and cytotoxicity of some 2-(5-nitro-2-furyl)-1,3,4-thiadiazole derivatives

被引：63

作者：

Foroumadi, A ^{[1
]}

Asadipour, A ^{[1
]}

Mirzaei, M ^{[1
]}

Karimi, J ^{[1
]}

Emami, S ^{[1
]}

机构：

[1] Kerman Univ Med Sci, Fac Pharm, Dept Med Chem, Kerman, Iran

来源：

FARMACO | 2002年 / 57卷 / 09期

关键词：

antituberculosis agents; minimum inhibitory concentration; cytotoxicity;

D O I：

10.1016/S0014-827X(02)01277-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A new series of 2-(5-nitro-2-furyl)-1,3,4-thiadiazole-2-sulfide, sulfoxide and sulfones were synthesized and evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis strain H(37)Rv using the radiometric BACTEC 460-TB methodology. Active compounds were also screened by serial dilution to assess toxicity to a VERO cell line. The results indicate that some compounds exhibited a good antituberculosis activity and the ethylthio analogue (5b) was the most active compound (MIC = 0.78 mug ml(-1)). Also, the cytotoxic effects indicate that compound 5b was the least toxic compound. (C) 2002 Editions scientifiques et medicales Elsevier SAS. All rights reserved.

引用

页码：765 / 769

页数：5

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