Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
- Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
- 한영휘; 한민수; 신동윤; 송치만; 한호규
- antidepression; novel pharmaceutical; azetidine; CNS
- Issue Date
- Journal of medicinal chemistry
- VOL 55, NO 18, 8188-8192
- 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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