1. Identification of 1‐phenoxy‐3‐(piperazin‐1‐yl)propan‐2‐ol derivatives as novel triple reuptake inhibitors
- Author
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Ashrafuzzaman, Md., Ji, Su Hyun, Ahn, Hyomin, Chung, Hwan Won, Choi, Daeun, Park, Ju Jin, Go, Minji, Pyo, Jung In, Shafioul, Azam Sharif Mohammed, Lee, Duck‐Hyung, Chi, Sung‐Gil, Song, Chiman, Cheong, Chan Seong, and Han, Seo‐Jung
- 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 19exhibited the most potent inhibitory activities against all three monoamine neurotransmitter transporters and the IC50values of 19against SERT, NET, and DAT were determined. In addition, binding modes of 19with SERT, NET, and DAT were predicted by docking studies. Novel 1‐phenoxy‐3‐(piperazin‐1‐yl)propan‐2‐ol derivatives exhibited potent inhibitory activities against serotonin, norepinephrine, and dopamine transporters (SERT, NET, and DAT, respectively) simultaneously and thus, 1‐phenoxy‐3‐(piperazin‐1‐yl)propan‐2‐ol derivatives possessed potential as triple reuptake inhibitors. Compound 19possessed the most potent combination of SERT, NET, and DAT inhibitory activity with inhibition values greater than 60% for all three monoamine transporters.
- Published
- 2023
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