Synthesis and pharmacological evaluation of sulfone substituted HIV protease inhibitors

Article abstract of DOI:10.1016/S0960-894X(97)00031-0

The sulfonamide substituted pyranones (I) have recently been shown to be potent HIV protease inhibitors. We prepared a series of sulfone substituted analogs and compared their biological activities to those of the corresponding sulfonamide analogs. It was determined that although these compounds maintained activity as enzyme inhibitors, they showed somewhat diminished antiviral activity even though they may possess increased membrane permeability.