1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors

Christopher D Beadle; John Boot; Nicholas P Camp; Nancy Dezutter; Jeremy Findlay; Lorna Hayhurst; John J Masters; Roberta Penariol; Magnus W Walter

doi:10.1016/j.bmcl.2005.07.038

1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4432-7. doi: 10.1016/j.bmcl.2005.07.038.

Authors

Christopher D Beadle¹, John Boot, Nicholas P Camp, Nancy Dezutter, Jeremy Findlay, Lorna Hayhurst, John J Masters, Roberta Penariol, Magnus W Walter

Affiliation

¹ Eli Lilly and Company Ltd, Lilly Research Centre, Erl Wood Manor, Windlesham, Surrey, GU20 6PH, UK.

PMID: 16137883
DOI: 10.1016/j.bmcl.2005.07.038

Abstract

A novel series of 1-aryl-3,4-dihydro-1H-quinolin-2-ones have been discovered as potent and selective norepinephrine reuptake inhibitors. Efficient synthetic routes have been developed which allow for the multi-gram preparation of both final targets and advanced intermediates for SAR expansion.

MeSH terms

Chromatography, High Pressure Liquid
Neurotransmitter Uptake Inhibitors / chemistry
Neurotransmitter Uptake Inhibitors / pharmacology*
Norepinephrine / physiology*
Quinolines / chemistry*
Quinolines / pharmacology*
Structure-Activity Relationship

Substances

Neurotransmitter Uptake Inhibitors
Quinolines
Norepinephrine