Author/Authors :
James D. Rodgers III، نويسنده , , Barry L. Johnson، نويسنده , , Haisheng Wang، نويسنده , , Susan Erickson-Viitanen، نويسنده , , Ronald M. Klabe، نويسنده , , Lee Bacheler، نويسنده , , Beverly C. Cordova، نويسنده , , Chong-Hwan Chang، نويسنده ,
Abstract :
Cyclic ureas containing 3-aminoindazole P2/P2′ groups are extremely potent inhibitors of HIV protease. The parent 3-aminoindazole 6 showed a Ki × 0.01 nM but poor translation of enzyme activity to antiviral activity was observed. A series of 3-alkylaminoindazoles revealed that translation improved with increasing lipophilicity. An X-ray crystal structure of 6 bound to HIV protease was obtained.
