Nonpeptidic HIV protease inhibitors: 6-alkyl-5, 6-dihydroyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl, 5-methylphenyl trio) moiety: Antiviral activities and pharmacokinetic properties

Authors
Prasad, JVNV Boyer, FE Domagala, JM Ellsworth, EL Gajda, C Hagen, SE Markoski, LJ Tait, BD Lunney, EA Tummino, PJ Ferguson, D Holler, T Hupe, D Nouhan, C Gracheck, SJ VanderRoest, S Saunders, J Iyer, K Sinz, M Brodfuehrer, J
Citation
Jvnv. Prasad et al., Nonpeptidic HIV protease inhibitors: 6-alkyl-5, 6-dihydroyran-2-ones possessing achiral 3-(4-amino/carboxamide-2-t-butyl, 5-methylphenyl trio) moiety: Antiviral activities and pharmacokinetic properties, BIOORG MED, 9(11), 1999, pp. 1481-1486
Citations number
11
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
11
Year of publication
1999
Pages
1481 - 1486
Database
ISI
SICI code
0960-894X(19990607)9:11<1481:NHPI66>2.0.ZU;2-O
Abstract
Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-S Ph (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their a ntiviral activities. Both the enantiomers of inhibitor 15 were synthesized. The in vitro resistance profile, inhibitory activities against cytochrome P450 isozymes and pharmacokinetic properties of inhibitor 15S will be discu ssed. (C) 1999 Elsevier Science Ltd. All rights reserved.