Affiliation:
1. Chemical & Biological integrative Research Center Korea Institute of Science and Technology Seoul South Korea
2. Division of Bio‐Medical Science & Technology, KIST School University of Science and Technology Seoul South Korea
3. Department of Chemistry Sogang University Seoul South Korea
4. Department of Life Sciences Korea University Seoul South Korea
5. Computational Science Research Center Korea Institute of Science and Technology Seoul South Korea
Abstract
AbstractNovel 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.
Funder
Korea Institute of Science and Technology
National Research Council of Science and Technology
Korea Drug Development Fund
National Research Foundation