Abstract
An efficient combination solution-phase/solid-phase route enabling the diversification of the P1', P2', and P3 subsites of indinavir has been established. The synthetic sequence can facilitate the rapid generation of HIV protease inhibitors possessing more favorable pharmacokinetic properties as well as enhanced potencies. Multiple compound dosing in vivo may also accelerate the identification of potential drug candidates.
MeSH terms
-
Animals
-
Cell Line
-
Combinatorial Chemistry Techniques*
-
Dogs
-
HIV Protease / metabolism
-
HIV Protease Inhibitors / chemical synthesis
-
HIV Protease Inhibitors / chemistry*
-
HIV Protease Inhibitors / pharmacokinetics
-
HIV Protease Inhibitors / pharmacology
-
Humans
-
Indinavir / analogs & derivatives*
-
Indinavir / chemical synthesis
-
Indinavir / chemistry*
-
Indinavir / pharmacokinetics
-
Indinavir / pharmacology
-
Models, Molecular
-
Molecular Conformation
-
Molecular Structure
-
T-Lymphocytes
Substances
-
HIV Protease Inhibitors
-
Indinavir
-
HIV Protease