期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 24, 页码 7719-7725出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.09.095
关键词
Privileged structure; 2-Aminothiazole; Antimicrobial; MIC; MRSA
资金
- Office of the Dean, School of Pharmacy
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.
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