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Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2002 Sep 02; Vol. 12 (17), pp. 2419-22. - Publication Year :
- 2002
-
Abstract
- Indinavir analogues with blocked metabolism sites show highly improved pharmacokinetic profiles in animals. The cis-aminochromanol substituted analogues exhibited excellent potency against both the wild-type (NL4-3) virus and protease inhibitor-resistant HIV strains.
- Subjects :
- Animals
Area Under Curve
Dogs
Drug Resistance
HIV Protease drug effects
HIV Protease Inhibitors metabolism
HIV Protease Inhibitors pharmacokinetics
Humans
Indinavir metabolism
Indinavir pharmacokinetics
Inhibitory Concentration 50
Metabolic Clearance Rate
Structure-Activity Relationship
Tumor Cells, Cultured
HIV drug effects
HIV Protease Inhibitors chemical synthesis
Indinavir analogs & derivatives
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 12
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 12161147
- Full Text :
- https://doi.org/10.1016/s0960-894x(02)00424-9