Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1363696 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
A novel series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols, have been discovered by combining virtual and focused screening efforts with design techniques. Synthesis of the two diastereomeric isomers of the molecule followed by chiral resolution of each enantiomer revealed the (2R,3S)-isomer to be a potent norepinephrine reuptake inhibitor (IC50 = 28 nM) with excellent selectivity over the dopamine transporter and 13-fold selectivity over the serotonin transporter.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Callain Y. Kim, Paige E. Mahaney, Oliver McConnell, Yingru Zhang, Eric Manas, Douglas M. Ho, Darlene C. Deecher, Eugene J. Trybulski,