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Discovery and development of substituted thiadiazoles as inhibitors of Staphylococcus aureus Sortase A

Journal article
Authors Patrick M. Wehrli
Ivana Uzelac
Thomas Olsson
T. Jacso
Daniel Tietze
Johan Gottfries
Published in Bioorganic & Medicinal Chemistry
Volume 27
Issue 19
ISSN 0968-0896
Publication year 2019
Published at Department of Chemistry and Molecular Biology
Centre for antibiotic resistance research, CARe
Language en
Links dx.doi.org/10.1016/j.bmc.2019.11504...
Keywords Staphylococcus aureus, Sortase A, SrtA inhibitors, Anti-virulence drugs, Antimicrobial resistance, surface-proteins, side-chain, resistance, virulence, accuracy, phosphines, mechanism, bacteria, docking, target, Biochemistry & Molecular Biology, Pharmacology & Pharmacy, Chemistry
Subject categories Pharmacology, Biochemistry and Molecular Biology

Abstract

High-throughput screening of small-molecule libraries has led to the identification of thiadiazoles as a new class of inhibitors against Staphylococcus aureus sortase A (SrtA). N-(5-((4-nitrobenzyl) thio)-1,3,4-thiadiazol-2-yl)nicotinamide (IC50= 3.8 mu M) was identified as a potent inhibitor of SrtA after synthetic modification of hit compounds. Additional ligands developed in this study displayed affinities in the low micromolar range without affecting bacterial growth in vitro. The study also suggest a new mode of action through covalent binding to the active site cysteine.

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