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…

Index: 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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Citation Number: 2

Abstract

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– ...