Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT_2C receptor

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• 作者：Thomas O. Schrader^a ; ^{tschrader619@gmail.com} ; Michelle Kasem^a ; Albert Ren^a ; Konrad Feichtinger^a ; Bilal Al Doori^a ; Jing Wei^b ; Chunrui Wu^b ; Huong Dang^a ; Minh Le^a ; Joel Gatlin^a ; Kelli Chase^a ; Jenny Dong^a ; Kevin T. Whelan^a ; Carleton Sage^a ; Andrew J. Grottick^a ; Graeme Semple^a
• 关键词：5-HT2C agonists ; Lorcaserin ; Tetrahydroquinoline ; CNS drugs ; Tricyclic amines
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 December 2016
• 年：2016
• 卷：26
• 期：24
• 页码：5877-5882
• 全文大小：851 K
• 卷排序：26

文摘

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.