Design, synthesis and biological evaluation of LX2343 derivatives as neuroprotective agents for the treatment of Alzheimer's disease
文献类型：期刊论文
| 作者 | Sun, Guanglong1,2,3; Wang, Junwei3; Guo, Xiaodan1,2; Lei, Min1,2 ; Zhang, Yinan3; Wang, Xiachang3; Shen, Xu3; Hu, Lihong1,2,3
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2018-02-10 |
| 卷号 | 145页码:622-633 |
| 关键词 | LX2343 derivatives Neuroprotective agents Alzheimer's disease Structural modifications Structure-activity relationships |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2017.12.080 |
| 文献子类 | Article |
| 英文摘要 | A series of LX2343 derivatives were designed, synthesized and evaluated as neuroprotective agents for Alzheimer's disease (AD) in vitro. Most of the compounds displayed potent neuroprotective activities. Especially for compound A6, exhibited a remarkable EC50 value of 0.22 mu M. Further investigation demonstrated that compound A6 can significantly reduce A beta production and increase A beta clearance, and alleviate Tau hyperphosphorylation. Most importantly, compound A6 could ameliorate learning and memory impairments in APP/PS1 transgenic mice. The present study evidently showed that compound A6 is a potent neuroprotective agent and might serve as a promising lead candidate for the treatment of Alzheimer's disease. (C) 2018 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | OXIDATIVE STRESS ; GSK-3-BETA INHIBITORS ; SH-SY5Y CELLS ; APOPTOSIS ; POTENT ; MODEL ; HYPOTHESIS ; DEMENTIAS |
| 资助项目 | National Natural Science Foundation of China[81473110] ; National Natural Science Foundation of China[81773596] ; National Natural Science Foundation of China[81561148011] ; Natural Science Foundation of Jiangsu Higher Education Institutions[17KJA360004] ; Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education Institutions[00000000] ; Priority Academic Program Development of Jiangsu Higher Education Institutions[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000425198200048 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279908]  |
| 专题 | 上海中药现代化研究中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Shen, Xu; Hu, Lihong |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Nanjing Univ Chinese Med, Stake Key Lab Cultivat Base TCM Qual & Efficacy, Jiangsu Collaborat Innovat Ctr Chinese Med Resour, Jiangsu Key Lab Funct Subst Chinese Med,Sch Pharm, Nanjing 210023, Jiangsu, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Sun, Guanglong,Wang, Junwei,Guo, Xiaodan,et al. Design, synthesis and biological evaluation of LX2343 derivatives as neuroprotective agents for the treatment of Alzheimer's disease[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2018,145:622-633. |
| APA | Sun, Guanglong.,Wang, Junwei.,Guo, Xiaodan.,Lei, Min.,Zhang, Yinan.,...&Hu, Lihong.(2018).Design, synthesis and biological evaluation of LX2343 derivatives as neuroprotective agents for the treatment of Alzheimer's disease.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,145,622-633. |
| MLA | Sun, Guanglong,et al."Design, synthesis and biological evaluation of LX2343 derivatives as neuroprotective agents for the treatment of Alzheimer's disease".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 145(2018):622-633. |
入库方式： OAI收割
来源：上海药物研究所
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