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

Lydie Poitout; Valérie Brault; Carole Sackur; Sonia Bernetière; José Camara; Pascale Plas; Pierre Roubert

doi:10.1016/j.bmcl.2007.06.010

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

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4464-70. doi: 10.1016/j.bmcl.2007.06.010. Epub 2007 Jun 8.

Authors

Lydie Poitout¹, Valérie Brault, Carole Sackur, Sonia Bernetière, José Camara, Pascale Plas, Pierre Roubert

Affiliation

¹ Department of Medicinal Chemistry, Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, 91966 Les Ulis Cedex, France. lydie.poitout@ipsen.com

PMID: 17574418
DOI: 10.1016/j.bmcl.2007.06.010

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.

MeSH terms

Animals
Area Under Curve
Benzimidazoles / blood
Benzimidazoles / chemistry*
Benzimidazoles / pharmacology*
Blood-Brain Barrier
Brain / metabolism
Half-Life
Humans
Molecular Structure
Rats
Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Benzimidazoles
Receptor, Melanocortin, Type 4