| Title | Design and synthesis of irreversible depsipeptidyl human rhinovirus 3C protease inhibitors. | ||
| Author | Webber, S E; Marakovits, J T; Dragovich, P S; Prins, T J; Zhou, R; Fuhrman, S A; Patick, A K; Matthews, D A; Lee, C A; Srinivasan, B; Moran, T; Ford, C E; Brothers, M A; Harr, J E; Meador, J W 3rd; Ferre, R A; Worland, S T | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 2001-Oct |
| PMID | 11591501 | PMCID | -N/A- |
| Affiliation | 1.Pfizer Global Research and Development, La Jolla, 3565 General Atomics Court, San Diego, CA 92121, USA. swebber@anadyspharma.com. | ||
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).