Author/Authors :
Xiaoqi Chen، نويسنده , , Lin Li، نويسنده , , Dale J. Kempf، نويسنده , , Hing Sham، نويسنده , , Norman E. Wideburg، نويسنده , , Ayda Saldivar، نويسنده , , Sudthida Vasavanonda، نويسنده , , Kennan C. Marsh، نويسنده , , Edith McDonald، نويسنده , , Daniel W. Norbeck، نويسنده ,
Abstract :
The hexahydrofurofuranyloxy group was evaluated as a conformationally constrained P2 ligand for symmetry-based HIV protease inhibitors. A number of compounds showed nM level activity against HIV in MT4 cells and lower protein binding than the licensed protease inhibitor ritonavir. However, replacement of 5-thiazole of ritonavir with a furofuran caused a reduction of the bioavailability in vivo.
