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Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
- Han, Y.;
- Han, M.;
- Shin, D.;
- Song, C.;
- Hahn, H.-G.
Citations
WEB OF SCIENCE
47Citations
SCOPUS
48초록
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. © 2012 American Chemical Society.
키워드
antidepressant agent; azetidine derivative; fluoxetine; nisoxetine; vanoxerine; alkylation; animal experiment; area under the curve; article; controlled study; drug activity; drug bioavailability; drug design; drug half life; drug screening; drug synthesis; Grignard reaction; human; human cell; maximum plasma concentration; mouse; nonhuman; oxidation kinetics; substitution reaction; Swern oxidation; time to maximum plasma concentration; Animals; Antidepressive Agents; Azetidines; Behavior, Animal; Drug Design; HEK293 Cells; Humans; Inhibitory Concentration 50; Mice; Neurotransmitter Uptake Inhibitors
- 제목
- Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors
- 저자
- Han, Y.; Han, M.; Shin, D.; Song, C.; Hahn, H.-G.
- 발행일
- 2012-09
- 유형
- Article
- 권
- 55
- 호
- 18
- 페이지
- 8188 ~ 8192