Identification of a novel series of benzimidazoles as potent and selective antagonists of the human melanocortin-4 receptor |
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| Authors: | Poitout Lydie Brault Valérie Sackur Carole Bernetière Sonia Camara José Plas Pascale Roubert Pierre |
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| Institution: | Department of Medicinal Chemistry, Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, 91966 Les Ulis Cedex, France. lydie.poitout@ipsen.com |
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| 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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