Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors
- Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors
- 박정은; 송치만; 최기현; 심태보; 문봉진; 노은주
- Triple reuptake inhibitors; Monoamine; Reuptake; Depression; Antidepressant; Serotonin; Dopamine; Norepinephrine; Lactam
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 20, 5515-5518
- 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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