Synthesis of triazole-oxazolidinones via a one-pot reaction and evaluation of their antimicrobial activity

被引：119

作者：

Demaray, Jeffrey A. ^{[1
]}

Thuener, Jason E. ^{[1
]}

Dawson, Matthew N. ^{[1
]}

Sucheck, Steven J. ^{[1
]}

机构：

[1] Univ Toledo, Dept Chem, Toledo, OH 43606 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 17期

基金：

美国国家科学基金会;

关键词：

antimycobacterial; antibacterial; oxazolidinone; one-pot;

D O I：

10.1016/j.bmcl.2008.07.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

C-5-substituted triazole-oxazolidinones were synthesized using a bromide catalyzed cycloaddition between aryl isocyanates and epibromohydrin followed by a three-component Huisgen cycloaddition. The library of compounds was screened for antibacterial activity against Mycobacterium smegmatis ATCC 14468, Bacillus subtilis ATCC 6633, and Enterococcus faecalis ATCC 29212. Notably, the 3-(4-acetyl-phenyl)5-(1H-1,2,3-triazol-1-yl) methyl)-oxazolidin-2-one (18) showed an MIC of 1 mu g/mL against M. smegmatis ATCC 14468, fourfold lower than the MIC measured for isoniazid. Published by Elsevier Ltd.

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收藏

页码：4868 / 4871

页数：4

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