Design, synthesis, and systematic evaluation of 4-arylpiperazine- and 4-benzylpiperidine napthyl ethers as inhibitors of monoamine neurotransmitters reuptake.
Two series of 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers were designed based on structure-activity relationship (SAR) and docking model of reported monoamine neurotransmitters reuptake inhibitors. The compounds were synthesized in 3-simple steps and their biological activities were evaluated. Several compounds were proven to be potent inhibitors of serotonin and norepinephrine reuptake. Computer docking was performed to study the interaction of the most potent compound 35 with human serotonin transporter. The results of the analyses suggest that 4-arylpiperazine- and 4-benzylpiperidine naphthyl ethers might be promising antidepressants worthy of further studies.
['Paudel|Suresh|S|', 'Min|Xiao|X|', 'Acharya|Srijan|S|', 'Khadka|Daulat Bikram|DB|', 'Yoon|Goon|G|', 'Kim|Kyeong-Man|KM|', 'Cheon|Seung Hoon|SH|']
D000928:Antidepressive Agents D015195:Drug Design D057809:HEK293 Cells D006801:Humans D062105:Molecular Docking Simulation D009638:Norepinephrine D000077489:Piperazine D010880:Piperidines D012701:Serotonin D050486:Serotonin Plasma Membrane Transport Proteins D017367:Serotonin Uptake Inhibitors D000068760:Serotonin and Noradrenaline Reuptake Inhibitors
4-Benzylpiperidine Naphthyl ether Docking 4-Arylpiperazine Depression Norepinephrine reuptake inhibitor Serotonin reuptake inhibitor