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
收藏
页码：7719 / 7725
页数：7
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