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ID: ALA3098057
Journal: Bioorg Med Chem Lett
Title: (E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.
Authors: Kim JJ, Wood MR, Stachel SJ, de Leon P, Nomland A, Stump CA, McWherter MA, Schirripa KM, Moore EL, Salvatore CA, Selnick HG.
Abstract: A new class of CGRP receptor antagonists was identified by replacing the central amide of a previously identified anilide lead structure with ethylene, ethane, or ethyne linkers. (E)-Alkenes as well as alkynes were found to preserve the proper bioactive conformation of the amides, necessary for efficient receptor binding. Further exploration resulted in several potent compounds against CGRP-R with low susceptibility to P-gp mediated efflux.
CiteXplore: 24332093