ChemInform Abstract: Aromatic P1 Replacements for the Highly Potent HIV-1 Protease Inhibitor Crixivan

A series of analogs of CRIXIVAN® containing various aromatic P1 ligands were prepared and evaluated for inhibition of the HIV-1 protease enzyme. These new compounds were found to be effective inhibitors at nanomolar concentrations in the in vitro enzyme inhibition assay as well as the whole cell assay.