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Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. doi: 10.1016/j.bmcl.2010.07.021. Epub 2010 Aug 17.

Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors.

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  • 1Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea.


A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In vivo models were used to evaluate the compound 19r for antidepressive, anxiolytic, and analgesic activity.

Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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