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

页码：2597 / 2600

页数：4

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