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ID: ALA1141621
Journal: Bioorg Med Chem Lett
Title: Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Authors: Chang LL, Yang GX, McCauley E, Mumford RA, Schmidt JA, Hagmann WK.
Abstract: The integrin VLA-4 is implicated in several inflammatory disease states. In search of non-peptidic antagonists of VLA-4, rotational constraints were imposed on the amide bond of prototypical N-sulfonylated dipeptide VLA-4 antagonists. By judicious structural modification of the side chains, trisubstituted imidazoles with moderate binding potencies were obtained, for example, 19, VLA-4 IC(50)=237 nM.
CiteXplore: 18242984