2. Academic Validation
  3. Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists

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

  • Bioorg Med Chem Lett. 2013 Oct 15;23(20):5684-8. doi: 10.1016/j.bmcl.2013.08.031.
George Tora 1,  Andrew P Degnan,  Charles M Conway,  Walter A Kostich,  Carl D Davis,  Sokhom S Pin,  Richard Schartman,  Cen Xu,  Kimberly A Widmann,  John E Macor,  Gene M Dubowchik
Affiliations

Affiliation

  • 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.
PMID: 23993336 DOI: 10.1016/j.bmcl.2013.08.031
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Several new potent CGRP Receptor antagonists have been prepared in which the amide bond of lead compound 1 has been replaced by bioisosteric imidazole moieties.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.

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