Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase

Authors
Corbett, JW Kresge, KJ Pan, SL Cordova, BC Klabe, RM Rodgers, JD Erickson-Viitanen, SK
Citation
Jw. Corbett et al., Trifluoromethyl-containing 3-alkoxymethyl- and 3-aryloxymethyl-2-pyridinones are potent inhibitors of HIV-1 non-nucleoside reverse transcriptase, BIOORG MED, 11(3), 2001, pp. 309-312
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
309 - 312
Database
ISI
SICI code
0960-894X(20010212)11:3<309:T3A3>2.0.ZU;2-8
Abstract
3-Alkoxymethyl- and 3-aryloxymethyl-2-pyridinones were synthesized and eval uated for activity as non-nucleoside reverse transcriptase inhibitors (NNRT Is) of HIV-I. It was found that several compounds were potent inhibitors of HIV-I with the most potent compound 24 exhibiting an IC90 = 32 nM. Compoun d 24 also possessed a potent resistance profile as demonstrated by submicro molar IC(90)s against several clinically meaningful mutant virus strains. ( C) 2001 DuPont Pharmaceuticals Company. Published by Elsevier Science Ltd. All rights reserved.