Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents

被引：70

作者：

Bairwa, Ranjeet ^{[1
]}

Kakwani, Manoj ^{[1
]}

Tawari, Nilesh R. ^{[1
]}

Lalchandani, Jaya ^{[1
]}

Ray, M. K. ^{[2
]}

Rajan, M. G. R. ^{[2
]}

Degani, Mariam S. ^{[1
]}

机构：

[1] Inst Chem Technol, Bombay 400019, Maharashtra, India

[2] Tata Mem Hosp Annex, Bhabha Atom Res Ctr, Radiat Med Ctr, Bombay 400012, Maharashtra, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 05期

关键词：

Cinnamic acid; Guanylhydrazone; Phenylacrylamide; Antitubercular; ANTIMYCOBACTERIAL EVALUATION; MYCOBACTERIUM-TUBERCULOSIS; LIPOPOLYSACCHARIDE;

D O I：

10.1016/j.bmcl.2010.01.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In an attempt to identify potential new agents active against tuberculosis, 20 novel phenylacrylamide derivatives incorporating cinnamic acids and guanylhydrazones were synthesized using microwave assisted synthesis. Activity of the synthesized compounds was evaluated using resazurin microtitre plate assay (REMA) against Mycobacterium tuberculosis H37Rv. Based on empirical structure-activity relationship data it was observed that both steric and electronic parameters play major role in the activity of this series of compounds. Compound 7s (2E)-N-((-2-(3,4-dimethoxybenzylidene) hydrazinyl) (imino) methyl)-3-(4-methoxyphenyl) acrylamide showed MIC of 6.49 mu M along with good safety profile of >50-fold in VERO cell line. Thus, this compound could act as a potential lead for further antitubercular studies. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1623 / 1625

页数：3

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