3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors

An T Vu; Stephen T Cohn; Eugene A Terefenko; William J Moore; Puwen Zhang; Paige E Mahaney; Eugene J Trybulski; Igor Goljer; Rebecca Dooley; Jenifer A Bray; Grace H Johnston; Jennifer Leiter; Darlene C Deecher

doi:10.1016/j.bmcl.2009.03.054

3-(Arylamino)-3-phenylpropan-2-olamines as a new series of dual norepinephrine and serotonin reuptake inhibitors

Bioorg Med Chem Lett. 2009 May 1;19(9):2464-7. doi: 10.1016/j.bmcl.2009.03.054. Epub 2009 Mar 18.

Authors

An T Vu¹, Stephen T Cohn, Eugene A Terefenko, William J Moore, Puwen Zhang, Paige E Mahaney, Eugene J Trybulski, Igor Goljer, Rebecca Dooley, Jenifer A Bray, Grace H Johnston, Jennifer Leiter, Darlene C Deecher

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.

PMID: 19329313
DOI: 10.1016/j.bmcl.2009.03.054

Abstract

A series of 3-(arylamino)-3-phenylpropan-2-olamines was prepared and screened for their ability to inhibit monoamine reuptake. A number of analogues displayed significant dual norepinephrine and serotonin reuptake inhibition. Compounds in this class exhibited minimal affinity for the dopamine transporter.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adrenergic Uptake Inhibitors / pharmacology
Animals
Chemistry, Pharmaceutical / methods*
Dogs
Dopamine Plasma Membrane Transport Proteins / antagonists & inhibitors*
Dopamine Plasma Membrane Transport Proteins / chemistry
Drug Design
Humans
Inhibitory Concentration 50
Ligands
Models, Chemical
Norepinephrine / antagonists & inhibitors*
Propanolamines / chemical synthesis*
Propanolamines / pharmacology
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
Selective Serotonin Reuptake Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Adrenergic Uptake Inhibitors
Dopamine Plasma Membrane Transport Proteins
Ligands
Propanolamines
Serotonin Uptake Inhibitors
Norepinephrine