title: Pulvinones as bacterial cell wall biosynthesis inhibitors.
abstract: Pulvinones were synthesized (>180) in arrays and evaluated as inhibitors of early stage cell wall biosynthesis enzymes MurA-MurD. Several pulvinones inhibited Mur enzymes with IC(50)'s in the 1-10 microg/mL range and demonstrated antibacterial activity against Gram-positive bacteria including methicillin-resistant Staphyloccus aureus, vancomycin-resistant Enterococcus faecalis, and penicillin-resistant Streptococcus pneumoniae.
authors.affiliation: Medicinal Chemistry, Chemical and Screening Sciences, Wyeth Research, Princeton, NJ 08543, USA. antanes@wyeth.com
authors.forename: Schuyler
authors.initials: S
authors.lastname: Antane
authors.forename: Craig E
authors.initials: CE
authors.lastname: Caufield
authors.forename: William
authors.initials: W
authors.lastname: Hu
authors.forename: David
authors.initials: D
authors.lastname: Keeney
authors.forename: Pornpen
authors.initials: P
authors.lastname: Labthavikul
authors.forename: Koi
authors.initials: K
authors.lastname: Morris
authors.forename: Shaughnessy M
authors.initials: SM
authors.lastname: Naughton
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Petersen
authors.forename: Beth A
authors.initials: BA
authors.lastname: Rasmussen
authors.forename: Guy
authors.initials: G
authors.lastname: Singh
authors.forename: Youjun
authors.initials: Y
authors.lastname: Yang
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000494:pharmacology; D002264:Carboxylic Acids / Q000138:chemical synthesis*; D002473:Cell Wall / Q000187:drug effects / Q000378:metabolism; D024881:Drug Resistance, Bacterial; D013293:Enterococcus faecalis / Q000378:metabolism; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000138:chemical synthesis*; D008712:Methicillin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D010406:Penicillins / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000378:metabolism; D013296:Streptococcus pneumoniae / Q000378:metabolism*; D014640:Vancomycin / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D002264:Carboxylic Acids; D007783:Lactones; D010406:Penicillins; D014640:Vancomycin; C492654:pulvinic acid; D008712:Methicillin