Synthesis and biological evaluation of novel 3, 4-diaryl lactam derivatives as triple reuptake inhibitors

J Park, C Song, K Choi, T Sim, B Moon…

文献索引：Park, Jung-Eun; Song, Chiman; Choi, Keehyun; Sim, Taebo; Moon, Bongjin; Roh, Eun Joo Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5515 - 5518

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被引用次数: 2

摘要

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 (IC 50= 14 nM) which was used as reference compound for dopamine transporter. In addition, 2a and 2b showed inhibition (5.17 μM– ...