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Synthesis and biological activity of (±)-7,3′,4′-trihydroxyhomoisoflavan and its analogs
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-11-06 , DOI: 10.1016/j.bmcl.2020.127674
Toshiro Noshita 1 , Kentaro Fujita 2 , Takeru Koga 2 , Hidekazu Ouchi 3 , Akihiro Tai 4
Affiliation  

Acetylcholinesterase (AChE) inhibitors and neurite outgrowth promoters are thought to alleviate the symptoms of degenerative brain disorders, such as Alzheimer's disease. We designed and synthesized a series of homoisoflavonoids based on the structure of natural homoisoflavan isolated from Dracaena cambodiana dragon’s blood. The homoisoflavonoids were then evaluated as AChE inhibitors and neurite outgrowth promoters. The catechol structure of the homoisoflavan B rings was important for AChE inhibition, and some of the homoisoflavonoids significantly promoted neurite outgrowth induced by nerve growth factor (NGF).



中文翻译:

(±)-7,3',4'-三羟基高异黄酮及其类似物的合成及生物学活性

乙酰胆碱酯酶(AChE)抑制剂和神经突增生促进剂被认为可减轻变性性脑部疾病的症状,例如阿尔茨海默氏病。基于从龙血树龙血中分离得到的天然异黄酮的结构,我们设计并合成了一系列异黄酮。然后将同型异黄酮评估为AChE抑制剂和神经突增生促进剂。高异黄烷B环的儿茶酚结构对于AChE抑制很重要,并且一些高异黄酮能显着促进神经生长因子(NGF)诱导的神经突生长。

更新日期:2020-11-06
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