Author/Authors :
Christopher T. Baker، نويسنده , , Francesco G. Salituro، نويسنده , , John J. Court، نويسنده , , David D. Deininger، نويسنده , , Eunice E. Kim، نويسنده , , Biquin Li، نويسنده , , Perry M. Novak، نويسنده , , Bhisetti G. Rao، نويسنده , , S. Pazhanisamy، نويسنده , , Wayne C. Schairer، نويسنده , , Roger D. Tung، نويسنده ,
Abstract :
A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors bearing a structurally novel backbone. Detailed structural analysis of several inhibitors prepared in this series has suggested that rigidification of the P1/P2 region of this class of molecules may result in compounds with improved potency.