Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA

被引：43

作者：

Annadurai, Sivakumar ^{[1
]}

Martinez, Rogelio ^{[1
]}

Canney, Daniel J. ^{[1
]}

Eidem, Tess ^{[2
]}

Dunman, Paul M. ^{[2
]}

Abou-Gharbia, Magid ^{[1
]}

机构：

[1] Temple Univ, Sch Pharm, Moulder Ctr Drug Discovery Res, Philadelphia, PA 19122 USA

[2] Univ Rochester, Med Ctr, Sch Med & Dent, Rochester, NY USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 24期

关键词：

Privileged structure; 2-Aminothiazole; Antimicrobial; MIC; MRSA; CONVENIENT COUPLING REAGENT; DISCOVERY;

D O I：

10.1016/j.bmcl.2012.09.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Privileged structure-based libraries have been shown to provide high affinity lead compounds for a variety of important biological targets. The present study describes the synthesis and screening of a 2-aminothiazole based compound library to determine their utility as antimicrobials, focusing on MRSA. Several of the compounds in this series demonstrated improved antimicrobial activity as compared to ceftriaxone (CTX), a beta-lactam antibiotic. The most potent compound (21) had MICs in the range of 24 mu g/ml across a panel of Staphylococcus aureus strains. In addition, trifluoromethoxy substituted aminothiazoles and aminobenzothiazoles were found to be potent antimicrobials with MICs of 2-16 mu g/ml. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：7719 / 7725

页数：7

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