P. Ettmayer et al., NOVEL, EXTENDED TRANSITION-STATE MIMIC IN HIV-1 PROTEASE INHIBITORS WITH PERIPHERAL C-2-SYMMETRY, Bioorganic & medicinal chemistry letters, 4(24), 1994, pp. 2851-2856
Extension of hydroxyethylene containing transition state mimics in HIV
-protease inhibitors by carboxy or hydroxymethyl substituents led to p
otent competitive enzyme inactivation as well as inhibition of HIV-1 r
eplication in MT4-cells. Two diastereomeric series are discussed.