Abstract
Conformationally-constrained macrocyclic peptide-based hydroxyethylamines, with 17- to 19-membered ring systems, have been designed and synthesized as HIV protease inhibitors. Structure-activity relationships were consistent with molecular modeling studies, and certain cyclic inhibitors were developed with HIV protease IC 50 values of ∼1 nM, and antiviral activities (HIV-1/RF infected MT-2 cells) of EC 50 4–8 nM.
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