Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors |
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| Authors: | Jung-eun Park Chiman Song Keehyun Choi Taebo Sim Bongjin Moon Eun Joo Roh |
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| Institution: | 1. Chemical Kinomics Research Center, Korea Institute of Science and Technology, Wolsong-gil 5, Seongbuk-gu, Seoul, Republic of Korea;2. Department of Chemistry, Sogang University, Baekbeomno 35, Mapogu, Seoul, Republic of Korea |
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| Abstract: | A series of 3,4-diarylpyrrolidin-2-one was designed, prepared and evaluated as triple reuptake inhibitors for antidepressant. Most compounds exhibited comparable in vitro efficacy as norepinephrine and dopamine transporter reuptake inhibitors. Especially, 2i showed better potency than GBR-12909 (IC50 = 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM–85.6 nM) for three transporters. |
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| Keywords: | Triple reuptake inhibitors Monoamine Reuptake Depression Antidepressant Serotonin Dopamine Norepinephrine Lactam |
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