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  • Title: Solid-phase synthesis and structure-activity relationships of novel biarylethers as melanin-concentrating hormone receptor-1 antagonists.
    Author: Ma V, Bannon AW, Baumgartner J, Hale C, Hsieh F, Hulme C, Rorrer K, Salon J, van Staden C, Tempest P.
    Journal: Bioorg Med Chem Lett; 2006 Oct 01; 16(19):5066-72. PubMed ID: 16887348.
    Abstract:
    Melanin-concentrating hormone (MCH) is a cyclic 19 amino acid orexigenic neuropeptide. The action of MCH on feeding is thought to involve the activation of its respective G protein-coupled receptor MCH-R1. Consequently, antagonists that block MCH regulated MCH-R1 activity may provide a viable approach to the treatment of diet-induced obesity. This communication reports the discovery of a novel MCH-R1 receptor antagonist, the biarylether 7, identified through high throughput screening. The solid-phase synthesis and structure-activity relationship of related analogs is described.
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