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: [email protected].
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.