title: Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.
abstract: Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA) infections are growing global health concerns. Structure-activity relationships of phenylthiazoles as a new antimicrobial class have been addressed. We present 10 thiazole derivatives that exhibit strong activity against 18 clinical strains of MRSA and VRSA with acceptable PK profile. Three derivatives revealed an advantage over vancomycin by rapidly eliminating MRSA growth within 6 h, and no derivatives are toxic to HeLa cells at 11 μg/mL.
authors.affiliation: Department of Comparative Pathobiology, Purdue University College of Veterinary Medicine , West Lafayette, Indiana 47906, United States.
authors.forename: Haroon
authors.initials: H
authors.lastname: Mohammad
authors.forename: Abdelrahman S
authors.initials: AS
authors.lastname: Mayhoub
authors.forename: Adil
authors.initials: A
authors.lastname: Ghafoor
authors.forename: Muhammad
authors.initials: M
authors.lastname: Soofi
authors.forename: Ruba A
authors.initials: RA
authors.lastname: Alajlouni
authors.forename: Mark
authors.initials: M
authors.lastname: Cushman
authors.forename: Mohamed N
authors.initials: MN
authors.lastname: Seleem
mesh_terms: D055808:Drug Discovery; D004352:Drug Resistance, Microbial; D009682:Magnetic Resonance Spectroscopy; D008712:Methicillin / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000494:pharmacology*; D014640:Vancomycin / Q000494:pharmacology*
chemical_list: D013844:Thiazoles; D014640:Vancomycin; D008712:Methicillin