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

Bioorg Med Chem Lett

Chemical Kinomics Research Center, Korea Institute of Science and Technology, Seoul 136-791, Republic of Korea. Electronic address:

Published: August 2014

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.

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http://dx.doi.org/10.1016/j.bmcl.2014.06.026DOI Listing

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