取代肼基甲硫酰胺作为有效的抗结核药物：合成与定量构效关系（QSAR）
Substituted hydrazinecarbothioamide as potent antitubercular agents: synthesis and quantitative structure-activity relationship (QSAR).
作者信息
Singh Supriya, Mandal Pintu K, Singh Nagendra, Misra Anup K, Singh Shubhra, Chaturvedi Vinita, Sinha Sudhir, Saxena Anil K
机构信息
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India.
出版信息
Bioorg Med Chem Lett. 2010 Apr 15;20(8):2597-600. doi: 10.1016/j.bmcl.2010.02.081. Epub 2010 Feb 23.
A series of novel substituted hydrazinecarbothioamides was synthesized and evaluated for anti-TB activity. Three most active compounds viz. 1, 6 and 12 were found to exhibit minimum inhibitory concentration (MIC) of 0.4 microg/mL, whereas four compounds viz. 3, 5, 10 and 11 showed comparatively lesser activity with MIC value of 0.8 microg/mL against Mycobacterium tuberculosis strain. A highly significant QSAR equation explaining 81.8% variance is described.
合成了一系列新型取代肼基碳硫酰胺并评估其抗结核活性。发现三种活性最高的化合物，即1、6和12，其最低抑菌浓度（MIC）为0.4微克/毫升，而四种化合物，即3、5、10和11，对结核分枝杆菌菌株的活性相对较低，MIC值为0.8微克/毫升。描述了一个解释81.8%方差的高度显著的定量构效关系（QSAR）方程。
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