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Bioorg Med Chem Lett. 2016 Jul 15;26(14):3216-3219. doi: 10.1016/j.bmcl.2016.05.079. Epub 2016 May 28.

New halogenated tris-(phenylalkyl)amines as h5-HT2B receptor ligands.

Author information

1
Chemistry Dept., Hunter College, City University Of New York, 695 Park Ave, New York, NY 10065, USA; CUNY Graduate Center, 365 5th Avenue, New York, NY 10016, USA.
2
Chemistry Dept., Hunter College, City University Of New York, 695 Park Ave, New York, NY 10065, USA.

Abstract

A series of compounds in which various halogen substituents were incorporated into a phenyl ring of a tris-(phenylalkyl)amine scaffold, was synthesized and evaluated for affinity to h5-HT2 receptors. In general, all compounds were found to have good affinity for the 5-HT2B receptor and were selective over 5-HT2A and 5-HT2C receptors. Compound 9i was the most selective compound in this study and is the highest affinity 5-HT2B receptor ligand bearing a tris-(phenylalkyl)amine scaffold to date.

KEYWORDS:

5-HT(2A); 5-HT(2B); CNS; Tris-(phenylalkyl)amine

PMID:
27261181
DOI:
10.1016/j.bmcl.2016.05.079
[Indexed for MEDLINE]

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