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新型N-苯基-N'-[4-(5-烷基/芳氨基-1,3,4-噻二唑-2-基)苯基]硫脲的合成及其抗结核活性

Synthesis and antituberculosis activity of new N-phenyl-N'-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thioureas.

作者信息

Karakuş S, Rollas S

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Haydarpaşa, Istanbul, Turkey.

出版信息

Farmaco. 2002 Jul;57(7):577-81. doi: 10.1016/s0014-827x(02)01252-1.

Abstract

In this study, eight original N-phenyl-N'-[4-(5-alkyl/arylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea derivatives were synthesized and tested for antituberculosis activity. Antituberculosis activities of the synthesized compounds were screened in vitro using BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv at 6.25 microg/ml. The highest inhibition observed with the synthesized compounds is 67% for N-phenyl-N'-[4-(5-cyclohexylamino-1,3,4-thiadiazole-2-yl)phenyl]thiourea.

摘要

在本研究中,合成了8种新型N-苯基-N'-[4-(5-烷基/芳氨基-1,3,4-噻二唑-2-基)苯基]硫脲衍生物,并对其抗结核活性进行了测试。使用BACTEC 460放射测量系统,在体外以6.25微克/毫升的浓度对合成化合物针对结核分枝杆菌H37Rv的抗结核活性进行了筛选。合成化合物中观察到的最高抑制率为N-苯基-N'-[4-(5-环己基氨基-1,3,4-噻二唑-2-基)苯基]硫脲的67%。

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