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

Title
Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors
Authors
박정은송치만최기현심태보문봉진노은주
Keywords
Triple reuptake inhibitors; Monoamine; Reuptake; Depression; Antidepressant; Serotonin; Dopamine; Norepinephrine; Lactam
Issue Date
2013-10
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 23, NO 20, 5515-5518
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.
URI
http://pubs.kist.re.kr/handle/201004/46559
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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