4.7 Article

Nitroisobenzofuranone, a small molecule inhibitor of multidrug-resistant Staphylococcus aureus, targets peptidoglycan biosynthesis

Journal

CHEMICAL COMMUNICATIONS
Volume 58, Issue 83, Pages 11669-11672

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d2cc04102b

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The study presents an in situ lactonization mechanism that generates a unique inhibitor, IITK2020, targeting antimicrobial resistance in S. aureus. This inhibitor shows effectiveness in inhibiting peptidoglycan biosynthesis and is active against multidrug-resistant clinical strains of S. aureus.
Antimicrobial resistance (AMR) is a global health concern. Targetting AMR, we present an in situ lactonization mechanism generating 4-nitroisobenzofuran-1(3H)-one (IITK2020), an exclusive S. aureus inhibitor at 2-4 mu g mL(-1) MIC including multidrug-resistant S. aureus clinical strains, that prevents peptidoglycan biosynthesis.

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