Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor. Issue 24 (15th December 2016)

• Record Type: Journal Article
• Authors: Schrader, Thomas O.; Kasem, Michelle; Ren, Albert; Feichtinger, Konrad; Al Doori, Bilal; Wei, Jing; Wu, Chunrui; Dang, Huong; Le, Minh; Gatlin, Joel; Chase, Kelli; Dong, Jenny; Whelan, Kevin T.; Sage, Carleton; Grottick, Andrew J.; Semple, Graeme
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 24(2016)
• Page Start: 5877
• Page End: 5882
• Publication Date: 2016-12-15
• Subjects: 5-HT2C agonists -- Lorcaserin -- Tetrahydroquinoline -- CNS drugs -- Tricyclic amines; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.11.016
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: The syntheses, structure-activity relationships (SARs), and biological activities of tetrahydroquinoline-based tricyclic amines as 5-HT2C receptor agonists are reported. An early lead containing a highly unique 6, 6, 7-ring system was optimized for both in vitro potency and selectivity at the related 5-HT2B receptor. Orally bioactive, potent, and selective 6, 6, 6-tricyclic 5-HT2C agonists were identified.