ArticleChemMedChem2020
Asymmetric Disulfanylbenzamides as Irreversible and Selective Inhibitors of Staphylococcus aureus Sortase A.
Article in ChemMedChem, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 34 citations in OpenAlex.
- A microscale thermophoresis-based enzymatic RNA methyltransferase assay enables the discovery of DNMT2 inhibitors.Communications chemistry · 2025Article
- Bacteria from the Amycolatopsis genus associated with a toxic bird secrete protective secondary metabolites.Nature communications · 2024Article
- Investigation of the Compatibility between Warheads and Peptidomimetic Sequences of Protease Inhibitors-A Comprehensive Reactivity and Selectivity Study.International journal of molecular sciences · 2023Article
- Identification of novel small-molecular inhibitors of Staphylococcus aureus sortase A using hybrid virtual screening.The Journal of antibiotics · 2022Article
- A low-cost 3D-printable differential scanning fluorometer for protein and RNA melting experiments.HardwareX · 2022Article
- Covalent sortase A inhibitor ML346 preventsRSC medicinal chemistry · 2022Article
- Identification of Novel Antistaphylococcal Hit Compounds Targeting Sortase A.Molecules (Basel, Switzerland) · 2021Article
- Bacterial adhesion to biomaterials: What regulates this attachment? A review.The Japanese dental science review · 2021Review
- GNPS-guided discovery of xylacremolide C and D, evaluation of their putative biosynthetic origin and bioactivity studies of xylacremolide A and B.RSC advances · 2021Article
- 2-Sulfonylpyrimidines as Privileged Warheads for the Development ofFrontiers in molecular biosciences · 2021Article
- Taxifolin, an Inhibitor of Sortase A, Interferes With the Adhesion of Methicillin-ResistantFrontiers in microbiology · 2021Article
- Asymmetric Disulfanylbenzamides as Irreversible and Selective Inhibitors of Staphylococcus aureus Sortase A.ChemMedChem · 2020Article
- New Cysteine Protease Inhibitors: Electrophilic (Het)arenes and Unexpected Prodrug Identification for theMolecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
12 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Staphylococcus aureus is one of the most frequent causes of nosocomial and community-acquired infections, with drug-resistant strains being responsible for tens of thousands of deaths per year. S. aureus sortase A inhibitors are designed to interfere with virulence determinants. We have identified disulfanylbenzamides as a new class of potent inhibitors against sortase A that act by covalent modification of the active-site cysteine. A broad series of derivatives were synthesized to derive structure-activity relationships (SAR). In vitro and in silico methods allowed the experimentally observed binding affinities and selectivities to be rationalized. The most active compounds were found to have single-digit micromolar K
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.