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ID: ALA1133803
Journal: Bioorg Med Chem Lett
Title: Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors.
Authors: Webber SE, Marakovits JT, Dragovich PS, Prins TJ, Zhou R, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Srinivasan B, Moran T, Ford CE, Brothers MA, Harr JE, Meador JW, Ferre RA, Worland ST.
Abstract: Novel tripeptidyl C-terminal Michael acceptors with an ester replacement of the P(2)-P(3) amide bond were investigated as irreversible inhibitors of the human rhinovirus (HRV) 3C protease (3CP). When screened against HRV serotype-14 the best compound was shown to have very good 3CP inhibition (k(obs)/[I]=270,000M(-1)s(-1)) and potent in vitro antiviral activity (EC(50)=7.0nM).
CiteXplore: 11591501