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

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

  • Bioorg Med Chem Lett. 2010 Sep 15;20(18):5567-71. doi: 10.1016/j.bmcl.2010.07.021.
Ki-Ho Lee 1,  Chun-Eung Park,  Kyung-Hyun Min,  Yong-Je Shin,  Coo-Min Chung,  Hui-Ho Kim,  Hae-Jeoung Yoon,  Won-Kim,  Eun-Ju Ryu,  Yu-Jin Shin,  Hyun-Sik Nam,  Jeong-Woo Cho,  Hee-Yoon Lee
Affiliations

Affiliation

  • 1 Department of Chemistry, Korea Advanced Institute of Science and Technology, Daejeon 305-701, Republic of Korea. [email protected]
PMID: 20724153 DOI: 10.1016/j.bmcl.2010.07.021
Abstract

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.

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