Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates

被引：79
作者：
Foroumadi, A [1 ]
Kargar, Z
Sakhteman, A
Sharifzadeh, Z
Feyzmohammadi, R
Kazemi, M
Shafiee, A
机构：
[1] Univ Tehran Med Sci, Fac Pharm, Tehran, Iran
[2] Univ Tehran Med Sci, Pharmaceut Sci Res Ctr, Tehran, Iran
[3] Kerman Univ Med Sci, Fac Pharm, Kerman, Iran
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 05期
关键词：
Mycobacterium tuberculosis; nitroimidazole; nitrofuran; nitrothiophene; 1,3,4-thiadiazole;
D O I：
10.1016/j.bmcl.2005.11.087
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two series of 2- and 3-[5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio, sulfinyl and sulfonyl] propionic acid alkyl esters were synthesized and screened for antituberculosis activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system. The MIC values for the compounds showing more than 90% inhibition were determined. The result of comparison between two groups of data exhibited that among the synthesized derivatives, the compound propyl 3-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-ylthio]propionate was the most active one (MIC = 1.56 mu g ml(-1)). (C) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1164 / 1167
页数：4
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