Synthesis and evaluation of 4-hydroxyl aurone derivatives as multifunctional agents for the treatment of Alzheimer's disease.
作者： Yan Li , Xiaoming Qiang , Li Luo , Yuxing Li , Ganyuan Xiao
DOI: 10.1016/J.BMC.2016.04.012
关键词:
摘要: A series of 4-hydroxyl aurone derivatives were designed synthesized and evaluated as potential multifunctional agents for the treatment Alzheimer's disease. The results demonstrated that most exhibited good properties. Among them, compound 14e displayed inhibitory activities self- Cu(2+)-induced Aβ1-42 aggregation with 99.2% 84.0% at 25μM, respectively, high antioxidant activity a value 1.90-fold Trolox. In addition, also showed remarkable both monoamine oxidase B IC50 values 0.271μM 0.393μM, respectively. However 6-methoxyl aurones 15a-c revealed excellent selectivity toward MAO-B. Furthermore, representative compounds 15b metal-chelating abilities blood-brain barrier (BBB) permeabilities in vitro.
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