HIV‐1 protease inhibitors containing a novel C₂ symmetrical hydroxyalkylgem‐diamino core structure

Two series of peptidomimetics containing a novel C 2 symmetrical hydroxyalkylgem‐diamino core structure were prepared, from amino acid starting materials, and evaluated as inhibitors of HIV‐1 protease (HIV‐1 Pr). 1, 1‐Diamino‐3‐hydroxypropane (gHse) derivatives showed weak inhibitory potency (IC 50 > 10 μM). In the 1, 1‐diamino‐2‐hydroxyethane (gSer) series, a compound containing P1/P1’benzyl and P2/P2’Fmoc substitueras, displayed a significant HIV‐1 Pr inhibition (IC 50 = 440 nM).