5,6-cis-Penems: Broad-Spectrum Anti-Methicillin-Resistant Staphylococcus aureus β-Lactam Antibiotics
- 1 July 1997
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 40 (14) , 2126-2132
- https://doi.org/10.1021/jm9703348
Abstract
5,6-cis-Penem derivatives have been synthesized and evaluated as anti-MRSA antibiotics. The cis-penems 5 and 6 showed potent activities against not only MRSA but also a wide variety of bacteria including beta-lactamase-producing microorganisms. These compounds were designed to have high affinity to the penicillin-binding protein 2a of MRSA and to form stable acyl intermediates with beta-lactamases by blocking the deacylating water molecule.Keywords
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