Bioorg Med Chem Lett. 2007 Aug 15;17(16):4464-70. Epub 2007 Jun 8.

Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.

Poitout L, Brault V, Sackur C, Bernetière S, Camara J, Plas P, Roubert P.

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Department of Medicinal Chemistry, Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, 91966 Les Ulis Cedex, France. lydie.poitout@ipsen.com

Abstract

A novel series of benzimidazoles was identified and optimized, leading to the discovery of potent and selective antagonists of the human melanocortin-4 receptor. In addition, compound 5i was shown to cross the blood-brain barrier after intravenous dosing in rats.

PMID:: 17574418; [PubMed - indexed for MEDLINE]

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