探索新型 3-取代氮杂环丁烷衍生物作为三重再摄取抑制剂。
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.
机构信息
Organic Chemistry Laboratory, Korea Institute of Science and Technology, Seoul 136-791, Korea.
出版信息
J Med Chem. 2012 Sep 27;55(18):8188-92. doi: 10.1021/jm3008294. Epub 2012 Sep 11.
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.
新型基于 3-芳基-3-氧代丙胺支架的氮杂环丁烷被设计、合成并评估为 TRIs。化合物 1 还原，然后 Swern 氧化，再格氏反应得到 3。3 的烷基化提供了相应的氮杂环丁烷衍生物 6，其中根据其生物学特征，从 86 种制备的类似物中选择了最有前途的两种，即 6bd 和 6be。化合物 6be 在 FST 中在 10mg/kg IV 或 20-40mg/kg PO 时具有体内活性。
Zotero 插件