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.

Article Details

Citation

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
DrugTargetPropertyMeasurementpHTemperature (°C)
AtomoxetineSodium-dependent noradrenaline transporterIC 50 (nM)3N/AN/ADetails
AtomoxetineSodium-dependent serotonin transporterIC 50 (nM)48N/AN/ADetails
DesipramineSodium-dependent noradrenaline transporterIC 50 (nM)3.4N/AN/ADetails
FluoxetineSodium-dependent serotonin transporterIC 50 (nM)9.4N/AN/ADetails
MazindolSodium-dependent dopamine transporterIC 50 (nM)22.1N/AN/ADetails