A set of HIV protease inhibitors represented by compound 2 has previously b
een described. Structural and conformational analysis of this compound sugg
ested that conformational restriction of the P-1/P-2 portion of the molecul
e could lead to a novel set of potent protease inhibitors. Thus, probe comp
ounds 3-7 were designed, synthesized, and found to be potent inhibitors of
HIV protease. (C) 1998 Elsevier Science Ltd. All rights reserved.