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Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor.
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.
Affiliation
  • Schrader TO; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA. Electronic address: tschrader619@gmail.com.
  • Kasem M; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Ren A; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Feichtinger K; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Al Doori B; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Wei J; WuXi AppTec (Wuhan) Co Ltd., 666 Gaoxin Road, East Lake High-tech Development Zone, Wuhan 430075, China.
  • Wu C; WuXi AppTec (Wuhan) Co Ltd., 666 Gaoxin Road, East Lake High-tech Development Zone, Wuhan 430075, China.
  • Dang H; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Le M; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Gatlin J; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Chase K; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Dong J; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Whelan KT; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Sage C; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Grottick AJ; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Semple G; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 26(24): 5877-5882, 2016 12 15.
Article in En | MEDLINE | ID: mdl-27864071
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Receptor, Serotonin, 5-HT2C / Serotonin 5-HT2 Receptor Agonists / Amines Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Quinolines / Receptor, Serotonin, 5-HT2C / Serotonin 5-HT2 Receptor Agonists / Amines Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2016 Document type: Article