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Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA).


ABSTRACT: Extending from a study we recently published examining the antitrypanosomal effects of a series of GroEL/ES inhibitors based on a pseudosymmetrical bis-sulfonamido-2-phenylbenzoxazole scaffold, here, we report the antibiotic effects of asymmetric analogs of this scaffold against a panel of bacteria known as the ESKAPE pathogens ( Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species). While GroEL/ES inhibitors were largely ineffective against K. pneumoniae, A. baumannii, P. aeruginosa, and E. cloacae (Gram-negative bacteria), many analogs were potent inhibitors of E. faecium and S. aureus proliferation (Gram-positive bacteria, EC50 values of the most potent analogs were in the 1-2 ?M range). Furthermore, even though some compounds inhibit human HSP60/10 biochemical functions in vitro (IC50 values in the 1-10 ?M range), many of these exhibited moderate to low cytotoxicity to human liver and kidney cells (CC50 values > 20 ?M).

SUBMITTER: Abdeen S 

PROVIDER: S-EPMC6345161 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature

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Sulfonamido-2-arylbenzoxazole GroEL/ES Inhibitors as Potent Antibacterials against Methicillin-Resistant Staphylococcus aureus (MRSA).

Abdeen Sanofar S   Kunkle Trent T   Salim Nilshad N   Ray Anne-Marie AM   Mammadova Najiba N   Summers Corey C   Stevens Mckayla M   Ambrose Andrew J AJ   Park Yangshin Y   Schultz Peter G PG   Horwich Arthur L AL   Hoang Quyen Q QQ   Chapman Eli E   Johnson Steven M SM  

Journal of medicinal chemistry 20180814 16


Extending from a study we recently published examining the antitrypanosomal effects of a series of GroEL/ES inhibitors based on a pseudosymmetrical bis-sulfonamido-2-phenylbenzoxazole scaffold, here, we report the antibiotic effects of asymmetric analogs of this scaffold against a panel of bacteria known as the ESKAPE pathogens ( Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter species). While GroEL/ES inhibitor  ...[more]

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