Synthesis and biological evaluation of novel 3,4-diaryl lactam derivatives as triple reuptake inhibitors This article is dedicated to Professor Jahyo Kang for his lifelong commitment to mentoring graduate students

Jung Eun Park, Chiman Song, Keehyun Choi, Taebo Sim, Bongjin Moon, Eun Joo Roh

Research output: Contribution to journalArticle

5 Citations (Scopus)

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-85.6 nM) for three transporters.

Original languageEnglish
Pages (from-to)5515-5518
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number20
DOIs
Publication statusPublished - 2013 Oct 15

Keywords

  • Antidepressant
  • Depression
  • Dopamine
  • Lactam
  • Monoamine
  • Norepinephrine
  • Reuptake
  • Serotonin
  • Triple reuptake inhibitors

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry
  • Molecular Medicine
  • Molecular Biology
  • Clinical Biochemistry
  • Biochemistry

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