Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis.
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.
Francisco
Gerardo D
GD
Chemical Sciences and Infectious Diseases, Wyeth Research, Pearl River, NY 10965, USA.
Li
Zhong
Z
Albright
J Donald
JD
Eudy
Nancy H
NH
Katz
Alan H
AH
Petersen
Peter J
PJ
Labthavikul
Pornpen
P
Singh
Guy
G
Yang
Youjun
Y
Rasmussen
Beth A
BA
Lin
Yang-I
YI
Mansour
Tarek S
TS
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
D000900:Anti-Bacterial Agents; D002219:Carbamates; D010457:Peptidoglycan; D010668:Phenylthiazolylthiourea