A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability

Abstract A new hydroxyethylamine class of inhibitors was designed combining features from our clinical candidate, L-735,524, along with small heterocyclic P 2 -ligands developed in these laboratories. Highly potent inhibitors possessing subnanomolar IC 50 's have been identified, which exhibit good antiviral potency in cell culture. L-738,872, a representative inhibitor in this class, showed 34% oral bioavailability in dogs.