title: Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis.
abstract: Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and PRSP. 3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria.
authors.affiliation: Chemical Sciences and Infectious Diseases, Wyeth Research, Pearl River, NY 10965, USA.
authors.forename: Gerardo D
authors.initials: GD
authors.lastname: Francisco
authors.forename: Zhong
authors.initials: Z
authors.lastname: Li
authors.forename: J Donald
authors.initials: JD
authors.lastname: Albright
authors.forename: Nancy H
authors.initials: NH
authors.lastname: Eudy
authors.forename: Alan H
authors.initials: AH
authors.lastname: Katz
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Petersen
authors.forename: Pornpen
authors.initials: P
authors.lastname: Labthavikul
authors.forename: Guy
authors.initials: G
authors.lastname: Singh
authors.forename: Youjun
authors.initials: Y
authors.lastname: Yang
authors.forename: Beth A
authors.initials: BA
authors.lastname: Rasmussen
authors.forename: Yang-I
authors.initials: YI
authors.lastname: Lin
authors.forename: Tarek S
authors.initials: TS
authors.lastname: Mansour
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002219:Carbamates / Q000737:chemistry* / Q000494:pharmacology*; D002473:Cell Wall / Q000187:drug effects / Q000201:enzymology; D013293:Enterococcus faecalis / Q000187:drug effects / Q000201:enzymology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D010457:Peptidoglycan / Q000096:biosynthesis*; D010668:Phenylthiazolylthiourea / Q000031:analogs & derivatives* / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects / Q000201:enzymology
chemical_list: D000900:Anti-Bacterial Agents; D002219:Carbamates; D010457:Peptidoglycan; D010668:Phenylthiazolylthiourea