title: Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
abstract: The synthesis and antimicrobial activity of several new 1-carba-1-dethiacephalosporins is described. The discovery of unique activity of some of the analogues against methicillin-resistant Staphylococcus aureus led to the development of a structure-activity relationship designed to optimize this activity. The results of this investigation along with the pharmacokinetic characteristics of select compounds are described.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285.
authors.forename: R J
authors.initials: RJ
authors.lastname: Ternansky
authors.forename: S E
authors.initials: SE
authors.lastname: Draheim
authors.forename: A J
authors.initials: AJ
authors.lastname: Pike
authors.forename: F W
authors.initials: FW
authors.lastname: Bell
authors.forename: S J
authors.initials: SJ
authors.lastname: West
authors.forename: C L
authors.initials: CL
authors.lastname: Jordan
authors.forename: C Y
authors.initials: CY
authors.lastname: Wu
authors.forename: D A
authors.initials: DA
authors.lastname: Preston
authors.forename: W
authors.initials: W
authors.lastname: Albron
authors.forename: J S
authors.initials: JS
authors.lastname: Kasher
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001798:Blood Proteins / Q000378:metabolism; D002511:Cephalosporins / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006207:Half-Life; D006801:Humans; D008253:Macaca mulatta; D008297:Male; D016106:Methicillin Resistance; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests; D051381:Rats; D017207:Rats, Sprague-Dawley; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001798:Blood Proteins; D002511:Cephalosporins