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Structure-activity Relationships Of N-substituted Piperazine Amine Reuptake Inhibitors.

M. Fray, G. Bish, P. V. Fish, A. Stobie, Florian Wakenhut, G. Whitlock
Published 2006 · Chemistry, Medicine

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We report the structure-activity relationships of further analogues in a series of piperazine derivatives as dual inhibitors of serotonin and noradrenaline reuptake, that is, with additional substitution of the phenyl rings, or their replacement by heterocycles. The enantiomers of compounds 1 and 2 were also profiled, and possessed drug-like physicochemical properties. In particular, compound (-)-2 lacked potent inhibitory activity against any of the important cytochromes P(450) and high selectivity over a wide range of receptors, which is unusual for a compound that inhibits human amine transporters.
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