HTS, chemical hybridization, and drug design identify a chemically unique antituberculosis agent-coupling serendipity and rational approaches to drug discovery

被引：27

作者：

Mao, Jialin

Wan, Baojie

Wang, Yuehong

Franzblau, Scott G.

Kozikowski, Alan P.

机构：

[1] Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago IL 60612

[2] Drug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, University of Illinois at Chicago, Chicago, IL 60612

来源：

CHEMMEDCHEM | 2007年 / 2卷 / 06期

关键词：

D O I：

10.1002/cmdc.200700048

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The high throughput screening of two chemical libraries against Mycobacterium tuberculosis led to the design of hybrid compounds by using nitrile oxide cycloaddition chemistry. One of the hybrids shows an excellent MIC against M. tuberculosis H37Rv. As this molecule shows no CYP3A4 inhibition and a maximum tolerated dose of ≥200 mgkg-1 po in mice, it represents a potential drug candidate for TB therapy. (Chemical Equation Presented) © 2007 Wiley-VCH Verlag GmbH& Co. KGaA.

引用

页码：811 / 813

页数：3

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