SYNTHESIS OF N-(HALOGENATED) BENZYL ANALOGS OF SUPERPOTENT SEROTONIN LIGANDS

In the last four years a group of extremely potent designer drugs, the N-benzylated phenylethylamines known as the NBOMe series, has surfaced on the street and in the news media. Although data documenting their high affinity and preference for 5-HT2 serotonin receptors abound (5-HT2A receptor activation is generally associated with the action of the "classical" hallucinogens), relatively little is known about the molecular basis of their potency and selectivity. In the setting of a project aiming to evaluate the possible involvement of halogen bonds in the binding of monoaminergic ligands to their receptors, we have begun to synthesize halogenated derivatives of known N-benzylated compounds for their pharmacological study. Here we report the synthesis of new phenylethylamine and tryptamine derivatives incorporating bromine atoms in their N-benzyl moiety.

Bibliographic Details

Main Authors:	TIRAPEGUI,CRISTIAN, TORO-SAZO,MIGUEL A, CASSELS,BRUCE K
Format:	Digital revista
Language:	English
Published:	Sociedad Chilena de Química 2014
Online Access:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072014000300022
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