Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Article Details
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Fray MJ, Bish G, Fish PV, Stobie A, Wakenhut F, Whitlock GA
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Bioorg Med Chem Lett. 2006 Aug 15;16(16):4349-53. Epub 2006 Jun 5.
- PubMed ID
- 16750363 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Duloxetine Sodium-dependent dopamine transporter IC 50 (nM) 870 N/A N/A Details Duloxetine Sodium-dependent noradrenaline transporter IC 50 (nM) 19 N/A N/A Details Duloxetine Sodium-dependent serotonin transporter IC 50 (nM) 6 N/A N/A Details Fluoxetine Sodium-dependent serotonin transporter IC 50 (nM) 16 N/A N/A Details