STUDIES ON ORALLY AVAILABLE INHIBITORS OF HIV PROTEASE - PEPTIDYL ALDEHYDES AND TRIFLUOROMETHYL KETONES

Authors
HODGE CN ALDRICH PE FERNANDEZ CH OTTO MJ RAYNER MM WONG YN ERICKSONVIITANEN S
Citation
Cn. Hodge et al., STUDIES ON ORALLY AVAILABLE INHIBITORS OF HIV PROTEASE - PEPTIDYL ALDEHYDES AND TRIFLUOROMETHYL KETONES, Antiviral chemistry & chemotherapy, 5(4), 1994, pp. 257-262
Citations number
31
Categorie Soggetti
Biology,"Pharmacology & Pharmacy
Journal title
Antiviral chemistry & chemotherapy → ACNP
ISSN journal
09563202
Volume
5
Issue
4
Year of publication
1994
Pages
257 - 262
Database
ISI
SICI code
0956-3202(1994)5:4<257:SOOAIO>2.0.ZU;2-Z
Abstract
Low-molecular-weight peptidyl aldehyde inhibitors of HIV protease that reach in vivo plasma concentrations after oral administration substan tially in excess of the antiviral IC90 are described. We also report e fforts to improve the potency and stability of these compounds that cu lminated in a series of peptidyl trifluoromethyl ketones with increase d potency but decreased bioavailability.