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

doi:10.1016/j.bmcl.2014.06.026

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^*

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-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 language	English
Pages (from-to)	3234-3237
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	24
Issue number	15
DOIs	https://doi.org/10.1016/j.bmcl.2014.06.026
Publication status	Published - 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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10.1016/j.bmcl.2014.06.026

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title = "Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors",

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.",

keywords = "3-Phenethylazetidines, Antidepressant, Depression, Triple reuptake inhibitor",

author = "Jun Yun and Minsoo Han and Chiman Song and Cheon, \{Seung Hoon\} and Kihang Choi and Hahn, \{Hoh Gyu\}",

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

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doi = "10.1016/j.bmcl.2014.06.026",

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T1 - Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors

AU - Yun, Jun

AU - Han, Minsoo

AU - Song, Chiman

AU - Cheon, Seung Hoon

AU - Choi, Kihang

AU - Hahn, Hoh Gyu

N1 - Funding Information: This work was supported by Korea Drug Development Fund and Korea Institute of Science and Technology .

PY - 2014/8/1

Y1 - 2014/8/1

N2 - 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.

AB - 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.

KW - 3-Phenethylazetidines

KW - Antidepressant

KW - Depression

KW - Triple reuptake inhibitor

UR - https://www.scopus.com/pages/publications/84904065583

U2 - 10.1016/j.bmcl.2014.06.026

DO - 10.1016/j.bmcl.2014.06.026

M3 - Article

C2 - 24974340

AN - SCOPUS:84904065583

SN - 0960-894X

VL - 24

SP - 3234

EP - 3237

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 15

ER -

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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