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. 2012 Apr 15;22(8):2917-21.
doi: 10.1016/j.bmcl.2012.02.065. Epub 2012 Mar 3.

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group

Guanglin Luo  1 , Ling Chen, Rita Civiello, Sokhom S Pin, Cen Xu, Walter Kostich, Michelle Kelley, Charles M Conway, John E Macor, Gene M Dubowchik
Affiliations

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group

Guanglin Luo et al. Bioorg Med Chem Lett. .

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.

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