Document Report Card

Basic Information

ID: ALA1146018

Journal: Bioorg Med Chem Lett

Title: The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.

Authors: Huck BR, Llamas L, Robarge MJ, Dent TC, Song J, Hodnick WF, Crumrine C, Stricker-Krongrad A, Harrington J, Brunden KR, Bennani YL.

Abstract: 5-HT2C agonists have shown efficacy in limiting food consumption and thus may serve as an important drug class in combating obesity. We describe the design and synthesis of a novel tricyclic single-nitrogen scaffold that was used to produce 5-HT2C agonists. SAR was developed around this chemotype and compounds were identified that were potent (Ki<15 nM) and selective relative to other 5-HT2 receptors. The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats.

CiteXplore: 16750364

DOI: 10.1016/j.bmcl.2006.04.070