Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors |
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Authors: | Fray M Jonathan Bish Gerwyn Fish Paul V Stobie Alan Wakenhut Florian Whitlock Gavin A |
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Affiliation: | Sandwich Chemistry, Pfizer Global Research and Development, Kent, UK. jonathan.fray@pfizer.com |
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Abstract: | 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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