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
收藏
页码：765 / 769
页数：5
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