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

鉴定一系列新型苯并咪唑作为人类黑皮质素-4受体的强效和选择性拮抗剂

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作者:Lydie Poitout, Valérie Brault, Carole Sackur, Sonia Bernetière, José Camara, Pascale Plas, Pierre Roubert

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.

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