Sham H L, Zhao C, Marsh K C, Betebenner D A, Lin S, Rosenbrook W, Herrin T, Li L, Madigan D, Vasavanonda S, Molla A, Saldivar A, McDonald E, Wideburg N E, Kempf D, Norbeck D W, Plattner J J
Abbott Laboratories, Abbott Park, Illinois 60064-3500, USA.
Biochem Biophys Res Commun. 1996 Aug 14;225(2):436-40. doi: 10.1006/bbrc.1996.1191.
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 incorporating polar functional groups at the P1' P2 and P2' positions. These compounds also possess good anti-viral activity by inhibition of the cytopathic effect of HIV-13B in MT-4 cells in vitro.