Author/Authors :
James D. Rodgers III، نويسنده , , Barry L. Johnson، نويسنده , , Haisheng Wang، نويسنده , , Roger A. Greenberg، نويسنده , , Susan Erickson-Viitanen، نويسنده , , Ronald M. Klabe، نويسنده , , Beverly C. Cordova، نويسنده , , Marlene M. Rayner، نويسنده , , Gilbert N. Lam، نويسنده , , Chong-Hwan Chang، نويسنده ,
Abstract :
A series of benzofused heterocycles was examined to replace the metabolically unstable benzyl alcohol P2/P2′ groups of DMP 323 (1). Extremely potent inhibitors of HIV protease (Ki < 0.01 nM) and excellent antiviral activity (IC90 = 8 nM) were found. An X-ray crystal structure of benzimidazolone 5a bound to HIV protease showed H-bonds to Asp30 and a bridging water molecule to Gly48.
