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

Autor:	Valerie Brault, Sonia Bernetiere, José Camara, Pascale Plas, Pierre Roubert, Lydie Poitout, Carole Sackur
Rok vydání:	2007
Předmět:	Benzimidazole Clinical Biochemistry Pharmaceutical Science Pharmacology Blood–brain barrier Biochemistry Structure-Activity Relationship chemistry.chemical_compound In vivo Drug Discovery medicine Animals Humans Structure–activity relationship Receptor Molecular Biology Molecular Structure Organic Chemistry Antagonist Brain Rats Melanocortin 4 receptor medicine.anatomical_structure chemistry Blood-Brain Barrier Area Under Curve Receptor Melanocortin Type 4 Molecular Medicine Benzimidazoles Melanocortin Half-Life
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:4464-4470
ISSN:	0960-894X
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd422ef705bb9e0089e5f9af72d36fe1 https://doi.org/10.1016/j.bmcl.2007.06.010 Zobrazit plný text záznamu Full Text from ScienceDirect