期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 25, 期 20, 页码 5278-5289出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.07.046
关键词
Benzylpiperidine-tetrazoles; Monoamine neurotransmitters; Serotonin; Norepinephrine and dopamine reuptake inhibitors; Docking
资金
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education [2012R1A1A2006613]
- [KRF-2017R1A2A2A05001227]
- National Research Foundation of Korea [2012R1A1A2006613] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
Monoamine transporters are important targets in the treatment of various central nervous disorders. Several limitations of traditional reuptake inhibitors, like delayed onset of action, insomnia, and sexual dysfunction, have compelled the search for safer, more effective compounds. In this study, we have sought to identify novel monoamine reuptake inhibitors. Based upon the docking study of compounds that we had reported previously, aromatic rings (A1) were modified to generate a novel series of benzylpiperidine-tetrazoles. Thirty-one compounds were synthesized and evaluated for their triple reuptake inhibition of serotonin, norepinephrine and dopamine. Triple reuptake inhibitor, compound 2q, in particular, showed potent serotonin reuptake inhibition, validating our design approach. (C) 2017 Elsevier Ltd. All rights reserved.
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