Indole-based peptidomimetic maleimides as SARS-CoV-2 Mpro inhibitor scaffolds compatible with reversible covalent inhibition: Warhead optimization and broad in vitro antiviral activity.
Although several SARS-CoV-2 main protease (Mpro) inhibitors have been clinically authorized, the continued evolution of SARS-CoV-2 and the emergence of resistance-associated mutations highlight the need for additional inhibitor scaffolds with balanced potency, chemical stability, and reversible covalent reactivity. Her...