Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors

Authors
Dragovich, PS Zhou, R Webber, SE Prins, TJ Kwok, AK Okano, K Fuhrman, SA Zalman, LS Maldonado, FC Brown, EL Meador, JW Patick, AK Ford, CE Brothers, MA Binford, SL Matthews, DA Ferre, RA Worland, ST
Citation
Ps. Dragovich et al., Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors, BIOORG MED, 10(1), 2000, pp. 45-48
Citations number
26
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
1
Year of publication
2000
Pages
45 - 48
Database
ISI
SICI code
0960-894X(20000103)10:1<45:SDOKTH>2.0.ZU;2-6
Abstract
Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rh inovirus 3C protease (3CP). An optimized example of such compounds displaye d potent 3CP inhibition activity (K-i = 0.0045 mu M) and in vitro antiviral properties (EC50 = 0.34 mu M) when tested against HRV serotype-14. (C) 199 9 Elsevier Science Ltd. All rights reserved.