Author/Authors :
Vu Ma، نويسنده , , Anthony W. Bannon، نويسنده , , Jamie Baumgartner، نويسنده , , Clarence Hale، نويسنده , , Faye Hsieh، نويسنده , , Christopher Hulme، نويسنده , , Kirk Rorrer، نويسنده , , John Salon، نويسنده , , Carlo van Staden، نويسنده , , Paul Tempest، نويسنده ,
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.