title: Propenylamide and propenylsulfonamide cephalosporins as a novel class of anti-MRSA beta-lactams.
abstract: 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.
authors.affiliation: Basilea Pharmaceutica International Ltd, CH-4005 Basel, Switzerland. jens.pohlmann@basilea.com
authors.forename: Jens
authors.initials: J
authors.lastname: Pohlmann
authors.forename: Natalya I
authors.initials: NI
authors.lastname: Vasilevich
authors.forename: Andrei I
authors.initials: AI
authors.lastname: Glushkov
authors.forename: Laurenz
authors.initials: L
authors.lastname: Kellenberger
authors.forename: Stuart
authors.initials: S
authors.lastname: Shapiro
authors.forename: Patrick
authors.initials: P
authors.lastname: Caspers
authors.forename: Malcolm G P
authors.initials: MG
authors.lastname: Page
authors.forename: Franck
authors.initials: F
authors.lastname: Danel
mesh_terms: D000577:Amides / Q000737:chemistry*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002511:Cephalosporins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects* / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D047090:beta-Lactams / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000577:Amides; D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D047090:beta-Lactams