The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT sub(2C) receptor agonist

5-HT sub(2C) 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-HT sub(2C) agonists. SAR was developed around this chemotype and compounds were identified that were potent (K sub(i) - 15 nM) and selective relative to other 5-HT sub(2) receptors. The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats.