Synthesis and biological evaluation of substituted 4,6-diarylpyrimidines and 3,5-diphenyl-4,5-dihydro-1H-pyrazoles as anti-tubercular agents

被引：39

作者：

Pathak, Vinay ^{[1
]}

Maurya, Hardesh K. ^{[1
]}

Sharma, Sandeep ^{[2
]}

Srivastava, Kishore K. ^{[2
]}

Gupta, Atul ^{[1
]}

机构：

[1] CSIR Cent Inst Med & Aromat Plants, Dept Med Chem, Lucknow 226015, Uttar Pradesh, India

[2] CSIR Cent Drug Res Inst, Div Microbiol, Lucknow 226031, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 13期

关键词：

4,6-Diarylpyrimidine; Pyrazole; Anti-tubercular; H37Rv; THP-1; cells; PYRIMIDINES; CHALCONES;

D O I：

10.1016/j.bmcl.2014.04.094

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Various substituted 4,6-diarylpyrimidin-2-amine (4), 4,6-diaryl-2-(heteroaryl)pyrimidine (6) and 1-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)ethanone (7) derivatives were synthesized in good yields using simple methodology. The synthesized compounds (4-7) were evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv strain. Compounds 4a, 6b, 7b, and 7c exhibited significant anti-tubercular activity at MIC values 25, 25, 12.5 and 12.5 mu M concentration. In vitro cytotoxicity data using non cancerous hepatic monocytes (THP-1) cells indicated that most active compounds 7b and 7c were safe as their MIC values were much lower than their cytotoxic values. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：2892 / 2896

页数：5

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