Abstract
The analogue that we chose to pursue can be conceptually derived from a Phe-Xaa dipeptide 1 by a series of rigidifying events (a) fixing the dihedral angle between the α and β carbons of phenylalanine; (b) blocking rotation of the side-chain phenyl group; and (c) fixing the directionality of the amide carbonyl group with respect to the indole ring and prohibiting C-N amide-bond rotation.
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