Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease

Authors
Dhanak, D Keenan, RM Burton, G Kaura, A Darcy, MG Shah, DH Ridgers, LH Breen, A Lavery, P Tew, DG West, A
Citation
D. Dhanak et al., Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease, BIOORG MED, 8(24), 1998, pp. 3677-3682
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
8
Issue
24
Year of publication
1998
Pages
3677 - 3682
Database
ISI
SICI code
0960-894X(199812)8:24<3677:BBRIOT>2.0.ZU;2-S
Abstract
A novel class of CMV protease inhibitors based on a benzothiopyran-S,S-diox ide nucleus has been discovered. Enzyme kinetic data supports a reversible mode of inhibition for a representative member of this class, 2-(3-pyridyl- N-oxide)benzothiopyran-4-one-S,S-dioxide, 1. Experiments in the presence an d absence of the disulfide reducing agent DTT suggest that the inhibition b y 1 is not due to oxidative inactivation of the enzyme. Also presented are results of some SAR studies of the benzothiopyranone ring system. (C) 1998 Elsevier Science Ltd. All rights reserved.