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某些烷基[5-(硝基芳基)-1,3,4-噻二唑-2-基硫代]丙酸酯的合成及其抗分枝杆菌活性

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

作者信息

Foroumadi Alireza, Kargar Zahra, Sakhteman Amirhossein, Sharifzadeh Zahra, Feyzmohammadi Robabeh, Kazemi Mahnoush, Shafiee Abbas

机构信息

Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1164-7. doi: 10.1016/j.bmcl.2005.11.087. Epub 2005 Dec 15.

Abstract

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 microgml(-1)).

摘要

合成了两系列2-和3-[5-(硝基芳基)-1,3,4-噻二唑-2-基硫代、亚磺酰基和磺酰基]丙酸烷基酯,并使用BACTEC 460放射性测定系统筛选了它们对结核分枝杆菌H37Rv的抗结核活性。测定了抑制率超过90%的化合物的最低抑菌浓度(MIC)值。两组数据的比较结果表明,在合成的衍生物中,化合物3-[5-(5-硝基噻吩-2-基)-1,3,4-噻二唑-2-基硫代]丙酸丙酯活性最高(MIC = 1.56微克/毫升)。

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