INHIBITION OF HUMAN RHINOVIRUS 3C PROTEASE BY HOMOPHTHALIMIDES

Authors
JUNGHEIM LN COHEN JD JOHNSON RB VILLARREAL EC WAKULCHIK M LONCHARICH RJ WANG QM
Citation
Ln. Jungheim et al., INHIBITION OF HUMAN RHINOVIRUS 3C PROTEASE BY HOMOPHTHALIMIDES, Bioorganic & medicinal chemistry letters, 7(12), 1997, pp. 1589-1594
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
12
Year of publication
1997
Pages
1589 - 1594
Database
ISI
SICI code
0960-894X(1997)7:12<1589:IOHR3P>2.0.ZU;2-E
Abstract
Homophthalimides 2a and 3a were found to be inhibitors of Rhinovirus 3 C protease through a blind screening effort. SAR studies resulted in c ompound 3g, which exhibited improved enzyme inhibition, in addition to whole cell antiviral activity. Molecular modeling studies suggest a p referred enzyme/inhibitor interaction, and LC/MS experiments confirmed tight/covalent binding of 3g to the enzyme. (C) 1997 Elsevier Science Ltd.