7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: Hit-to-lead optimization

Abstract New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT 2C receptor agonists. Appropriate substitution of the amino group (R 1 R 2 N–) gave compounds that were potent 5-HT 2C agonists with minimal activation of the 5-HT 2A and 5-HT 2B receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.