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

Poitout, L., Brault, V., Sackur, C., Bernetiere, S., Camara, J., Plas, P., Roubert, P.
Journal   Bioorg Med Chem Lett
Species  
Analytes Measured   cAMP
Matrix Tested   Cell lysates
Year   2007
Volume   17
Page Numbers   4464-70
Application   Phosphoproteins
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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