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Bioorg Med Chem Lett. 2013 Oct 15;23(20):5684-8. doi: 10.1016/j.bmcl.2013.08.031. Epub 2013 Aug 13.

Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.

Author information

1
Medicinal Chemistry, Molecular Sciences and Candidate Optimization, Bristol-Myers Squibb, 311 Pennington-Rocky Hill Road, Pennington, NJ 08534, USA. Electronic address: george.tora@bms.com.

Abstract

Several new potent CGRP receptor antagonists have been prepared in which the amide bond of lead compound 1 has been replaced by bioisosteric imidazole moieties. Substitution at N-1 of the imidazole was optimized to afford compounds with comparable potency to that of lead 1. Conformational restraint of the imidazole to form tetrahydroimidazo[1,5-a]pyrazine 43 gave substantially improved permeability.

KEYWORDS:

CGRP; CGRP receptor antagonists; Imidazoles; Migraine; Migraineurs

PMID:
23993336
DOI:
10.1016/j.bmcl.2013.08.031
[Indexed for MEDLINE]
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