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

Md Ashrafuzzaman, Su Hyun Ji, Hyomin Ahn, Hwan Won Chung, Daeun Choi, Ju Jin Park, Minji Go, Jung In Pyo, Azam Sharif Mohammed Shafioul, Duck Hyung Lee, Sung Gil Chi, Chiman Song, Chan Seong Cheong, Seo Jung Han

Research output: Contribution to journalArticlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)596-599
Number of pages4
JournalBulletin of the Korean Chemical Society
Volume44
Issue number7
DOIs
Publication statusPublished - 2023 Jul

Bibliographical note

Funding Information:
This research was supported by Korea Institute of Science and Technology (KIST), the National Research Council of Science & Technology (NST) grant from the Korea government (MSIT) (No. CPS21061‐100), and Korea Drug Development Fund funded by Ministry of Science and ICT, Ministry of Trade, Industry, and Energy, and Ministry of Health and Welfare (HN22C0063000022, Republic of Korea). In addition, this research was supported by the Technology Development Program to Solve Climate Change of the National Research Foundation (NRF) of Korea, funded by the Ministry of Science and ICT (NRF‐2020M1A2A2079798).

Publisher Copyright:
© 2023 Korean Chemical Society, Seoul & Wiley-VCH GmbH.

Keywords

  • antidepressants
  • aryloxypropanolpiperazine
  • major depressive disorder
  • monoamine neurotransmitter
  • triple reuptake inhibitor

ASJC Scopus subject areas

  • General Chemistry

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