Ketopiperazines:Conformationally Constrained Peptidomimetic of Arginine Amides

摘要

We have synthesized guanidine-containing ketopiperazines designed to be conformational mimics of peptidomimetic arginine amides.D-Allylglycine was converted by an efficient approach to give enantiopure ketopiperazines in which the trans stereochemistry of the C-substituents resulted from stereospecific enolate alkylation.It has long been recognized that biologically active peptides possess significant potential for drug development.