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Bioorg Med Chem Lett. 2016 Dec 15;26(24):5877-5882. doi: 10.1016/j.bmcl.2016.11.016. Epub 2016 Nov 9.

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor.

Author information

1
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA. Electronic address: tschrader619@gmail.com.
2
Department of Medicinal Chemistry, Arena Pharmaceuticals, 6154 Nancy Ridge Drive, San Diego, CA 92121, USA.
3
WuXi AppTec (Wuhan) Co Ltd., 666 Gaoxin Road, East Lake High-tech Development Zone, Wuhan 430075, China.

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.

KEYWORDS:

5-HT(2C) agonists; CNS drugs; Lorcaserin; Tetrahydroquinoline; Tricyclic amines

PMID:
27864071
DOI:
10.1016/j.bmcl.2016.11.016
[Indexed for MEDLINE]

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