Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA (TM))

Authors
Patel, M McHugh, RJ Cordova, BC Klabe, RM Erickson-Viitanen, S Trainor, GL Ko, SS
Citation
M. Patel et al., Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA (TM)), BIOORG MED, 9(22), 1999, pp. 3221-3224
Citations number
7
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
22
Year of publication
1999
Pages
3221 - 3224
Database
ISI
SICI code
0960-894X(19991115)9:22<3221:SAEOBA>2.0.ZU;2-R
Abstract
Two series of benzoxazinones differing in the aromatic substitution pattern were prepared and evaluated as HIV-1 reverse transcriptase inhibitors. The 5-fluoro (5a-d) and 6-nitro (5e-h) substituted compounds displayed activit y comparable or better than Efavirenz, the lead structure of the series. (C ) 1999 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. A ll rights reserved.