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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 ?g/mL.

SUBMITTER: Mohammad H 

PROVIDER: S-EPMC4353699 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature

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Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.

Mohammad Haroon H   Mayhoub Abdelrahman S AS   Ghafoor Adil A   Soofi Muhammad M   Alajlouni Ruba A RA   Cushman Mark M   Seleem Mohamed N MN  

Journal of medicinal chemistry 20140114 4


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 HeL  ...[more]

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