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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7719-25. doi: 10.1016/j.bmcl.2012.09.095. Epub 2012 Oct 3.

Design and synthesis of 2-aminothiazole based antimicrobials targeting MRSA.

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Temple University School of Pharmacy, Moulder Center for Drug Discovery Research, Philadelphia, PA, USA.


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

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