These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Discovery and development of substituted thiadiazoles as inhibitors of Staphylococcus aureus Sortase A.
    Author: Wehrli PM, Uzelac I, Olsson T, Jacso T, Tietze D, Gottfries J.
    Journal: Bioorg Med Chem; 2019 Oct 01; 27(19):115043. PubMed ID: 31420255.
    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 µM) 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.
    [Abstract] [Full Text] [Related] [New Search]