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ID: ALA1131817
Journal: Bioorg Med Chem Lett
Title: Structure-based design of irreversible, tripeptidyl human rhinovirus 3C protease inhibitors containing N-methyl amino acids.
Authors: Dragovich PS, Webber SE, Prins TJ, Zhou R, Marakovits JT, Tikhe JG, Fuhrman SA, Patick AK, Matthews DA, Ford CE, Brown EL, Binford SL, Meador JW, Ferre RA, Worland ST.
Abstract: Tripeptide-derived molecules incorporating N-methyl amino acid residues and C-terminal Michael acceptor moieties were evaluated as irreversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). Such compounds displayed good 3CP inhibition activity (k(obs)/[I] up to 610,000 M(-1) s(-1)) and potent in vitro antiviral properties (EC50 approaching 0.03 microM) when tested against HRV serotype-14.
CiteXplore: 10465543