Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA

Annadurai, Sivakumar and Martinez, Rogelio and Canney, Daniel J. and Eidem, Tess and Dunman, Paul M. and Abou-Gharbia, Magid (2012) Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA. Bioorganic & Medicinal Chemistry Letters, 22 (24). pp. 7719-7725. ISSN 0960894X


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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 b-lactam antibiotic. The most potent compound (21) had MICs in the range of 2– 4 lg/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 lg/ml.

Item Type: Article
Subjects: Pharmaceutical Sciences
Divisions: College of Pharmacy > Pharmaceutical Sciences
Depositing User: Dr Sivakumar Annadurai
Date Deposited: 01 May 2017 09:33
Last Modified: 01 May 2017 09:33

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