| Title | Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors. | ||
| Author | Dragovich, P S; Zhou, R; Webber, S E; Prins, T J; Kwok, A K; Okano, K; Fuhrman, S A; Zalman, L S; Maldonado, F C; Brown, E L; Meador, J W 3rd; Patick, A K; Ford, C E; Brothers, M A; Binford, S L; Matthews, D A; Ferre, R A; Worland, S T | ||
| Journal | Bioorg Med Chem Lett | Publication Year/Month | 2000-Jan |
| PMID | 10636240 | PMCID | -N/A- |
| Affiliation | 1.Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. psd@agouron.com. | ||
Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K = 0.0045 microM) and in vitro antiviral properties (EC50=0.34 microM) when tested against HRV serotype-14.