Design and synthesis of novel conformationally restricted HIV protease inhibitors

Abstract A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P 1 /P 2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3–7 were designed, synthesized, and found to be potent inhibitors of HIV protease.