NOVEL AZACYCLIC UREAS THAT ARE POTENT INHIBITORS OF HIV-1 PROTEASE

A series of novel, azacyclic ureas which are highly potent inhibitors of the HIV-1 protease (IC50 = 4.1 to <0.5 nM were synthesized. Aqueous solubilities of this series of compounds were improved by incorporati ng polar functional groups at the P-1' P-2 and P-2' positions. These c ompounds also possess good anti-viral activity by inhibition of the cy topathic effect of HIV-1(3B) in MT-4 Cells in vitro. (C) 1996 Academic Press, Inc.