SMALL PEPTIDIC ALDEHYDE INHIBITORS OF HUMAN RHINOVIRUS 3C PROTEASE

Authors
SHEPHERD TA COX GA MCKINNEY E TANG J WAKULCHIK M ZIMMERMAN RE VILLARREAL EC
Citation
Ta. Shepherd et al., SMALL PEPTIDIC ALDEHYDE INHIBITORS OF HUMAN RHINOVIRUS 3C PROTEASE, Bioorganic & medicinal chemistry letters, 6(23), 1996, pp. 2893-2896
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
23
Year of publication
1996
Pages
2893 - 2896
Database
ISI
SICI code
0960-894X(1996)6:23<2893:SPAIOH>2.0.ZU;2-X
Abstract
Small peptide aldehydes were designed to mimic the preferred substrate requirements for the human rhinovirus 3C protease. Di- and tripeptide aldehydes containing a methionine sulfone as a P-1 surrogate for glut amine show low micromolar enzyme inhibitory and antiviral tissue cultu re activity. LY338387, obtained in a short and efficient synthesis, ap pears to validate the protease as a therapeutic target. Copyright (C) 1996 Elsevier Science Ltd