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

Title
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
Authors
한영휘한민수신동윤송치만한호규
Keywords
antidepression; novel pharmaceutical; azetidine; CNS
Issue Date
2012-09
Publisher
Journal of medicinal chemistry
Citation
VOL 55, NO 18, 8188-8192
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.
URI
http://pubs.kist.re.kr/handle/201004/43130
ISSN
00222623
Appears in Collections:
KIST Publication > Article
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