Discovery of a new series of monoamine reuptake inhibitors, the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ols.

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 (IC(50)=28 nM) with excellent selectivity over the dopamine transporter and 13-fold selectivity over the serotonin transporter.

journal_name

Bioorg Med Chem Lett

authors

Kim CY,Mahaney PE,McConnell O,Zhang Y,Manas E,Ho DM,Deecher DC,Trybulski EJ

doi

10.1016/j.bmcl.2009.07.053

subject

Has Abstract

pub_date

2009-09-01 00:00:00

pages

5029-32

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01014-2

journal_volume

19

pub_type

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