Aromatic P1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN®

Abstract A series of analogs of CRIXIVAN ® containing various aromatic P 1 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.