2. Academic Validation
  3. Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors

Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors

  • J Med Chem. 2012 Sep 27;55(18):8188-92. doi: 10.1021/jm3008294.
Younghue Han 1,  Minsoo Han,  Dongyun Shin,  Chiman Song,  Hoh-Gyu Hahn
Affiliations

Affiliation

  • 1 Organic Chemistry Laboratory, Korea Institute of Science and Technology, Seoul 136-791, Korea.
PMID: 22938049 DOI: 10.1021/jm3008294
Abstract

Novel azetidines based on the 3-aryl-3-oxypropylamine scaffold were designed, synthesized, and evaluated as TRIs. Reduction of 1 followed by Swern oxidation and then Grignard reaction gave 3. The alkylation of 3 provided the corresponding azetidine derivatives 6, of which the two most promising, 6bd and 6be, were selected from 86 prepared analogues based on their biological profiles. Compound 6be showed activity in vivo in FST at 10 mg/kg IV or 20-40 mg/kg PO.

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