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Novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines as potent and selective agonists of the 5-HT2C receptor.
Schrader, Thomas O; Zhu, Xiuwen; Kasem, Michelle; Ren, Albert; Liu, Chunyan; Wu, Chunrui; Dang, Huong; Le, Minh; Gatlin, Joel; Chase, Kelli; Frazer, John; Whelan, Kevin T; Grottick, Andrew J; Hutton, Clayton; Barden, Jeremy; Chen, Chuan; Ortiz, Alvaro; Feichtinger, Konrad; 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.
  • Zhu X; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • 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.
  • Liu C; 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.
  • Frazer 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.
  • Grottick AJ; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Hutton C; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Barden J; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Chen C; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
  • Ortiz 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.
  • Semple G; Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 38: 127872, 2021 04 15.
Article in En | MEDLINE | ID: mdl-33636307
ABSTRACT
A series of novel (R)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,n]naphthyridines were identified as potent and selective agonists of the 5-HT2C receptor. Optimizations performed on a previously reported series of racemic tetrahydroquinoline-based tricyclic amines, delivered an advanced drug lead, (R)-4-(3,3,3-trifluoropropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine, which displayed excellent in vitro and in vivo pharmacological profiles.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptor, Serotonin, 5-HT2C / Serotonin 5-HT2 Receptor Agonists Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Receptor, Serotonin, 5-HT2C / Serotonin 5-HT2 Receptor Agonists Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article