title: Structure-activity relationships of novel potent MurF inhibitors.
abstract: A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers.
authors.affiliation: Infectious Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, 200 Abbott Park Road, Abbott Park, IL 60064, USA. yu-gui.y.gu@abbott.com
authors.forename: Yu Gui
authors.initials: YG
authors.lastname: Gu
authors.forename: Alan S
authors.initials: AS
authors.lastname: Florjancic
authors.forename: Richard F
authors.initials: RF
authors.lastname: Clark
authors.forename: Tianyuan
authors.initials: T
authors.lastname: Zhang
authors.forename: Curt S
authors.initials: CS
authors.lastname: Cooper
authors.forename: David D
authors.initials: DD
authors.lastname: Anderson
authors.forename: Claude G
authors.initials: CG
authors.lastname: Lerner
authors.forename: J Owen
authors.initials: JO
authors.lastname: McCall
authors.forename: Yingna
authors.initials: Y
authors.lastname: Cai
authors.forename: Candace L
authors.initials: CL
authors.lastname: Black-Schaefer
authors.forename: Geoffrey F
authors.initials: GF
authors.lastname: Stamper
authors.forename: Philip J
authors.initials: PJ
authors.lastname: Hajduk
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Beutel
mesh_terms: D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D010453:Peptide Synthases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D010457:Peptidoglycan / Q000096:biosynthesis; D013329:Structure-Activity Relationship
chemical_list: D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D010457:Peptidoglycan; D010453:Peptide Synthases; C060628:UDP-N-acetylmuramoylalanyl-D-glutamyllysine-D-alanyl-D-alanine ligase