| Title | Structure-based design of irreversible, tripeptidyl human rhinovirus 3C protease inhibitors containing N-methyl amino acids. | ||
| Author | Dragovich, P S; Webber, S E; Prins, T J; Zhou, R; Marakovits, J T; Tikhe, J G; Fuhrman, S A; Patick, A K; Matthews, D A; Ford, C E; Brown, E L; Binford, S L; Meador, J W 3rd; Ferre, R A; Worland, S T | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 1999-Aug |
| PMID | 10465543 | PMCID | -N/A- |
| Affiliation | 1.Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. | ||
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.