Effective use of phenyl and heterocyclic rings: Synthesis of inhibitors of HIV-RT and thrombin

Abstract

In two different programs to develop enzyme inhibitors for the treatment of HIV infection and abnormal thrombosis, we have effectively replaced aliphatic groups with pisystems: i.e. acetylenes, aromatic, and heterocyclic rings. This has led to an improvement in both the activity and pharmacokinetic properties of these compounds.