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Propenylamide and propenylsulfonamide cephalosporins as a novel class of anti-MRSA β-lactams

✍ Scribed by Jens Pohlmann; Natalya I. Vasilevich; Andrei I. Glushkov; Laurenz Kellenberger; Stuart Shapiro; Patrick Caspers; Malcolm G.P. Page; Franck Danel

Book ID: 104004486
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 419 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.05.110

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✦ Synopsis

Novel C(3) propenylamide and propenylsulfonamide cephalosporins have been synthesized and tested for their ability to inhibit the penicillin-binding protein 2' (PBP2') from Staphylococcus epidermidis and the growth of a panel of clinically relevant bacterial species, including methicillin-resistant Staphylococcus aureus (MRSA). The most potent compounds inhibited the growth of MRSA strains with minimum inhibitory concentrations (MIC) as low as 1 microg/mL. The structure-activity relationship revealed the potential for further optimization of this new cephalosporin class.

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