Thiophene-fused γ-lactams inhibit the SARS-CoV-2 main protease <i>via</i> reversible covalent acylation
Gayatri, Lennart Brewitz, Lewis T. Ibbotson, E. Salah, Shyam Basak, Hani Choudhry, Christopher J. Schofield
Abstract
Thiophene-fused γ-lactams are reversible covalent inhibitors of the SARS-CoV-2 main protease, a nucleophilic cysteine enzyme. γ-Lactams can inhibit nucleophilic cysteine enzymes by S -acylation as well as nucleophilic serine enzymes by O -acylation.
Topics & Concepts
AcylationNucleophileChemistryCysteineCovalent bondEnzymeSerine proteaseStereochemistryThiopheneSerineCysteine proteaseProteaseCombinatorial chemistryBiochemistryOrganic chemistryCatalysisClick Chemistry and ApplicationsHIV/AIDS drug development and treatmentPeptidase Inhibition and Analysis