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Bioorg Med Chem Lett. 2009 Apr 1;19(7):1871-5. doi: 10.1016/j.bmcl.2009.02.071. Epub 2009 Feb 21.

7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.

Author information

1
Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent CT13 9NJ, UK.

Abstract

New 7-sulfonamido-3-benzazepines 3 are disclosed as 5-HT(2C) receptor agonists. Appropriate substitution of the amino group (R(1)R(2)N-) gave compounds that were potent 5-HT(2C) agonists with minimal activation of the 5-HT(2A) and 5-HT(2B) receptors. Furthermore, representative examples had excellent in vitro ADME properties and good selectivity over ion channel activity.

PMID:
19269173
DOI:
10.1016/j.bmcl.2009.02.071
[Indexed for MEDLINE]

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