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Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
Younghue Han1, Minsoo Han, Dongyun Shin
1Organic Chemistry Laboratory, Korea Institute of Science and Technology, Seoul 136-791, Korea.
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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