Substituted hydrazinecarbothioamide as potent antitubercular agents: Synthesis and quantitative structure-activity relationship (QSAR)

被引：16
|
作者：
Singh, Supriya [1 ]
Mandal, Pintu K. [1 ]
Singh, Nagendra [1 ]
Misra, Anup K. [1 ]
Singh, Shubhra [2 ]
Chaturvedi, Vinita [2 ]
Sinha, Sudhir [2 ]
Saxena, Anil K. [1 ]
机构：
[1] Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226001, Uttar Pradesh, India
[2] Cent Drug Res Inst, Drug Target Discovery & Dev Div, Lucknow 226001, Uttar Pradesh, India
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 08期
关键词：
Tuberculosis; Hydrazinecarbothioamides; QSAR; Synthesis; MYCOBACTERIUM-TUBERCULOSIS; MACROPHAGES; AVIUM;
D O I：
10.1016/j.bmcl.2010.02.081
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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 mu g/mL, whereas four compounds viz. 3, 5, 10 and 11 showed comparatively lesser activity with MIC value of 0.8 mu g/mL against Mycobacterium tuberculosis strain. A highly significant QSAR equation explaining 81.8% variance is described. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2597 / 2600
页数：4
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