Basic Information
ID: ALA2021833
Journal: Bioorg Med Chem Lett
Title: Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.
Authors: Luo G, Chen L, Civiello R, Pin SS, Xu C, Kostich W, Kelley M, Conway CM, Macor JE, Dubowchik GM.
Abstract: In our continuing efforts to identify CGRP receptor antagonists that can be dosed orally for the treatment of migraine headache, we have investigated a pyridine bioisosteric replacement of a polar amide portion of a previous lead compound, BMS-694153. Pyridine derivatives were discovered and their SAR was studied. Some of them showed excellent binding potency. However, oral bioavailability was low, even for compounds with good Caco-2 cell permeability.
CiteXplore: 22429470
DOI: 10.1016/j.bmcl.2012.02.065
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets