Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors

Article abstract of DOI:10.1016/S0960-894X(98)00669-6

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.