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

Autor:	Peter J. Tummino, James Saunders, Stephen J. Gracheck, Bradley Dean Tait, J. V. N. Vara Prasad, Joanne I. Brodfuehrer, Christopher Andrew Gajda, Krishna R. Iyer, Tod P. Holler, Susan Elizabeth Hagen, Steven VanderRoest, Edmund L. Ellsworth, Fred E. Boyer, Carolyn Nouhan, Donna Ferguson, Larry James Markoski, Michael Sinz, Donald Hupe, Elizabeth A. Lunney, John M. Domagala
Rok vydání:	1999
Předmět:	Models Molecular Anti-HIV Agents Dihydropyran Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Thio Carboxamide Crystallography X-Ray Biochemistry Chemical synthesis Inhibitory Concentration 50 Mice Structure-Activity Relationship chemistry.chemical_compound Dogs Drug Discovery medicine Animals Moiety HIV Protease Inhibitor Molecular Biology Pyrans chemistry.chemical_classification biology Chemistry Organic Chemistry HIV Protease Inhibitors Kinetics Enzyme inhibitor biology.protein Molecular Medicine Lactone
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 9:1481-1486
ISSN:	0960-894X
Popis:	Dihydropyran-2-ones possessing amino and carboxamide functionalities on 3-SPh (2-tert-butyl, 5-methyl) ring were synthesized and evaluated for their antiviral 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 discussed.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::15d4105a46f0a7705446df6fa7d3c542 https://doi.org/10.1016/s0960-894x(99)00237-1 Zobrazit plný text záznamu Full Text from ScienceDirect