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Design, synthesis, and evaluation of genipin derivatives for the treatment of Alzheimer's Disease
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-11-28 , DOI: 10.1111/cbdd.13194 Weijun Huang 1 , Yujun Wang 1 , Jiaming Li 1 , Yanchun Zhang 1 , Xiaodong Ma 1 , Panhu Zhu 1 , Yang Zhang 1
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2018-11-28 , DOI: 10.1111/cbdd.13194 Weijun Huang 1 , Yujun Wang 1 , Jiaming Li 1 , Yanchun Zhang 1 , Xiaodong Ma 1 , Panhu Zhu 1 , Yang Zhang 1
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Twenty‐two novel genipin derivatives have been designed, synthesized, and evaluated for their inhibitory activity against acetylcholinesterase (AChE). As a result, compound 13a bearing ligustrazine moiety displayed the most potent AChE inhibitory activity in this series with IC50 value of 218 nm. Besides, MTT assay was performed to investigate the neuroprotection of these compounds against PC12 cells injured by Amyloid β‐protein 1–42 (Aβ1–42). Among them, 8a showed higher inhibition rate (%Inhibition = 22.29) than the positive reference Donepezil (%Inhibition = 17.65).
中文翻译：
Genipin衍生物的设计，合成和评估，用于治疗阿尔茨海默氏病
已经设计，合成并评估了22种新颖的Genipin衍生物对乙酰胆碱酯酶（AChE）的抑制活性。结果，带有川gust嗪部分的化合物13a在该系列中表现出最有效的AChE抑制活性，IC 50值为218 n m。此外，进行了MTT分析以研究这些化合物对淀粉样β蛋白1-42（Aβ1-42）损伤的PC12细胞的神经保护作用。其中8a的抑制率（％Inhibition = 22.29）比阳性对照多奈哌齐（％Inhibition = 17.65）高。
更新日期：2018-11-28
中文翻译：
Genipin衍生物的设计，合成和评估，用于治疗阿尔茨海默氏病
已经设计，合成并评估了22种新颖的Genipin衍生物对乙酰胆碱酯酶（AChE）的抑制活性。结果，带有川gust嗪部分的化合物13a在该系列中表现出最有效的AChE抑制活性，IC 50值为218 n m。此外，进行了MTT分析以研究这些化合物对淀粉样β蛋白1-42（Aβ1-42）损伤的PC12细胞的神经保护作用。其中8a的抑制率（％Inhibition = 22.29）比阳性对照多奈哌齐（％Inhibition = 17.65）高。
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