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Bioorg Med Chem Lett. 2016 Feb 15;26(4):1229-32. doi: 10.1016/j.bmcl.2016.01.026. Epub 2016 Jan 16.

Synthesis and SAR of calcitonin gene-related peptide (CGRP) antagonists containing substituted aryl-piperazines and piperidines.

Author information

1
Bristol-Myers Squibb Discovery, Bristol-Myers Squibb Research & Development, 5 Research Parkway, Wallingford, CT 06492, USA.

Abstract

Calcitonin gene-related peptide (CGRP) is a potent neuropeptide implicated in the pathophysiology of migraine. In the course of seeking CGRP antagonists with improved oral bioavailability, metabolic stability, and pharmacokinetic properties, lower molecular weight, structurally simpler piperidine and piperazine analogs of BMS-694153 were prepared. Several were found to have nM binding affinity in vitro. The synthesis and SAR of these substituted piperidine and piperazine CGRP antagonists are discussed.

KEYWORDS:

CGRP receptor antagonist; Calcitonin gene-related peptide (CGRP); Migraine headache

PMID:
26832218
DOI:
10.1016/j.bmcl.2016.01.026
[Indexed for MEDLINE]

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