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

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3234-7. doi: 10.1016/j.bmcl.2014.06.026.

Jun Yun ¹, Minsoo Han ², Chiman Song ², Seung Hoon Cheon ³, Kihang Choi ⁴, Hoh-Gyu Hahn ⁵

Affiliations

1 Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea; Department of Chemistry, Research Institute for Natural Sciences, Korea University, Seoul 136-701, Republic of Korea.
2 Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea.
3 College of Pharmacy, Chonnam National University, Gwangju 500-757, Republic of Korea.
4 Department of Chemistry, Research Institute for Natural Sciences, Korea University, Seoul 136-701, Republic of Korea.
5 Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea. Electronic address: hghahn@kist.re.kr.

PMID: 24974340 DOI: 10.1016/j.bmcl.2014.06.026

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.

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