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

Viral Rawat; Sona Tiwari; Shweta Khanna; Umang Gupta; Sridhar S N C; Dharmendra K Yadav; Grace Kaul; Abdul Akhir; Deepanshi Saxena; Saravanan Matheshwaran; Sidharth Chopra; Dharmaraja Allimuthu

doi:10.1039/d2cc04102b

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

Chem Commun (Camb). 2022 Oct 18;58(83):11669-11672. doi: 10.1039/d2cc04102b.

Authors

Affiliations

¹ Department of Chemistry, Indian Institute of Technology Kanpur, Uttar Pradesh 208016, India. atdharma@iitk.ac.in.
² Department of Biological Sciences and Bioengineering, Indian Institute of Technology Kanpur, Uttar Pradesh 208016, India.
³ Division of Molecular Microbiology and Immunology, CSIR-Central Drug Research Institute Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, Uttar Pradesh, India.
⁴ AcSIR: Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India.

PMID: 36172810
DOI: 10.1039/d2cc04102b

Abstract

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 μg mL^-1 MIC including multidrug-resistant S. aureus clinical strains, that prevents peptidoglycan biosynthesis.

MeSH terms

Anti-Bacterial Agents / pharmacology
Anti-Infective Agents* / pharmacology
Humans
Methicillin-Resistant Staphylococcus aureus*
Microbial Sensitivity Tests
Peptidoglycan
Staphylococcal Infections*
Staphylococcus aureus

Substances

Anti-Bacterial Agents
Anti-Infective Agents
Peptidoglycan