Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors

Jun Yun, Minsoo Han, Chiman Song, Seung Hoon Cheon, Kihang Choi, Hoh Gyu Hahn

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition profiles. Compound 2at showed most potent triple reuptake inhibitor with good selectivity as a candidate for depression.

Original languageEnglish
Pages (from-to)3234-3237
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number15
DOIs
Publication statusPublished - 2014 Aug 1

Keywords

  • 3-Phenethylazetidines
  • Antidepressant
  • Depression
  • Triple reuptake inhibitor

ASJC Scopus subject areas

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

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