Synthesis and antiviral activity of P1′ arylsulfonamide azacyclic urea HIV protease inhibitors

A series of novel azacyclic urea HIV protease inhibitors bearing a benzenesulfonamide group at P1′ were synthesized utilizing a parallel synthesis method. Structural studies of early analogs bound in the enzyme active site were used to design more potent inhibitors. The effects of substituting the P1′ benzenesulfonyl group on antiviral activity and protein binding are described.