3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors

Authors
Corbett, JW Pan, SL Markwalder, JA Cordova, BC Klabe, RM Garber, S Rodgers, JD Erickson-Viitanen, SK
Citation
Jw. Corbett et al., 3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors, BIOORG MED, 11(2), 2001, pp. 211-214
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
2
Year of publication
2001
Pages
211 - 214
Database
ISI
SICI code
0960-894X(20010122)11:2<211:3APN>2.0.ZU;2-L
Abstract
A series of unique 3,3a-dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones and a 2a,5-dihydro-2H-thieno[4,3,2-de]quinazoline-4(3H)-thione were found to be H IV-1 non-nucleoside reverse transcriptase inhibitors. One of these compound s, as the racemate, possessed an IC90 = 4.6 nM against wild-type virus in a whole cell antiviral assay and had an IC90 = 76 and 897 nM against the cli nically significant K103N and K103N/L100I mutant viruses, respectively. (C) 2001 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. Al l rights reserved.