Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates
Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates
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DOI：
10.1016/j.bmcl.2005.11.087
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发表时间：
2006-03-01
影响因子：
2.7
通讯作者：
Shafiee, A
中科院分区：
文献类型：
--
作者：
Foroumadi, A;Kargar, Z;Shafiee, A
合成了2-和3-[5-（硝基芳基）-1，3，4-噻二唑-2-硫基、亚磺酰基和磺酰基]丙酸烷基酯，并利用BACTEC 460放射活性测定系统对结核分枝杆菌H37 Rv进行了抗结核活性筛选。测定显示超过90%抑制的化合物的MIC值。两组数据的比较结果表明，在所合成的衍生物中，化合物3-[5-（5-硝基噻吩-2-基）-1，3，4-噻二唑-2-基硫代]丙酸丙酯是最有活性的一种（MIC = 1.56 μ g ml（-1））。(C)2005爱思唯尔有限公司保留所有权利。
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.