title: Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor.
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.
authors.affiliation: Department of Medicinal Chemistry, Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, 91966 Les Ulis Cedex, France. lydie.poitout@ipsen.com
authors.forename: Lydie
authors.initials: L
authors.lastname: Poitout
authors.forename: Valérie
authors.initials: V
authors.lastname: Brault
authors.forename: Carole
authors.initials: C
authors.lastname: Sackur
authors.forename: Sonia
authors.initials: S
authors.lastname: Bernetière
authors.forename: José
authors.initials: J
authors.lastname: Camara
authors.forename: Pascale
authors.initials: P
authors.lastname: Plas
authors.forename: Pierre
authors.initials: P
authors.lastname: Roubert
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001562:Benzimidazoles / Q000097:blood / Q000737:chemistry* / Q000494:pharmacology*; D001812:Blood-Brain Barrier; D001921:Brain / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D044105:Receptor, Melanocortin, Type 4 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D044105:Receptor, Melanocortin, Type 4