Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 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

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

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

George Tora et al. Bioorg Med Chem Lett. .

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Several new potent CGRP receptor antagonists have been prepared in which the amide bond of lead compound 1 has been replaced by bioisosteric imidazole moieties.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.

PubMed Disclaimer

MeSH terms

Substances

LinkOut - more resources