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

    10 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

    Bibliographical note

    Funding Information:
    This work was supported by Korea Drug Development Fund and Korea Institute of Science and Technology .

    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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