Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
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Zhang P, Terefenko EA, McComas CC, Mahaney PE, Vu A, Trybulski E, Koury E, Johnston G, Bray J, Deecher D
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6067-70. doi: 10.1016/j.bmcl.2008.10.026. Epub 2008 Oct 11.
- PubMed ID
- 18951020 [ View in PubMed]
- Abstract
A series of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors was discovered. Several compounds such as 15 and 20 showed good hNET potency. Compounds 15 and 20 also displayed excellent selectivity at hNET that appeared superior to those of reboxetine and atomoxetine (4 and 5).
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Atomoxetine Sodium-dependent noradrenaline transporter IC 50 (nM) 3 N/A N/A Details Atomoxetine Sodium-dependent serotonin transporter IC 50 (nM) 48 N/A N/A Details Desipramine Sodium-dependent noradrenaline transporter IC 50 (nM) 3.4 N/A N/A Details Fluoxetine Sodium-dependent serotonin transporter IC 50 (nM) 9.4 N/A N/A Details Mazindol Sodium-dependent dopamine transporter IC 50 (nM) 22.1 N/A N/A Details