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Identification of 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives as novel triple reuptake inhibitors


BULLETIN OF THE KOREAN CHEMICAL SOCIETY



Ji, SH  ( Ji, Su Hyun ) &  Lee, DH   (  Lee, Duck-Hyung  )



DOI: 10.1002/bkcs.12693  

Early Access  MAR 2023

index date    :   2023-04-19

Article Type :      Article, Early Access




Novel 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives were designed and synthesized as potential triple reuptake inhibitors, which simultaneously inhibit serotonin, norepinephrine, and dopamine transporters (SERT, NET, and DAT, respectively) . Through neurotransmitter transporter uptake assays, inhibitory activities of 1-phenoxy-3-(piperazin-1-yl)propan-2-ol derivatives were evaluated. We discovered compound 19 exhibited the most potent inhibitory activities against all three monoamine neurotransmitter transporters and the IC50 values ​​of 19 against SERT, NET, and DAT were determined. In addition, binding modes of 19 with SERT, NET, and DAT were predicted by docking studies.


https://onlinelibrary.wiley.com/doi/abs/10.1002/bkcs.12693


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