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| 1 | Multitarget therapeutic strategies for Alzheimer's disease显示文摘Neurodegenerative diseases such as Alzheimer's, Huntington's and Parkinson's diseases have multifaceted nature because of the different factors contributing to their progression. The complex nature of neurodegenerative diseases has developed a pressing need to design multitarget-directed ligands to address the complementary pathways involved in these diseases. The major enzyme targets for development of therapeutics for Alzheimer's disease are cholinesterase and β-secretase enzymes. In this review, we discuss recent advances in profiling single target inhibitors based on these enzymes to multitarget-directed ligands as potential therapeutics for this devastating disease. In addition, therapeutics based on iron chelation strategy are discussed as well. | Mostafa M.Ibrahim Moustafa T.Gabr | 2019 | Neural Regeneration Research2019，14，3： | 8 |
| 2 | Combining fatty acid amide hydrolase (FAAH) inhibition with peroxisome proliferator-activated receptor (PPAR) activation: a new potential multi-target therapeutic strategy for the treatment of Alzheimer’s disease显示文摘Alzheimer’s disease(AD)is a widespread pathology described for the first time by Alois Alzheimer in 1907.It can be classified as a neurodegenerative disease consisting in a progressive loss of memory and cognitive functions,whose prevalence is estimated to grow due to the increasing life expectancies all over the world.To date,the only treatments available for this disease are symptomatic and no actual effective cure is available.The main effect of the drugs commonly used in therapeutic protocols is to temporarily delay the onset of the disease and to slightly improve the patients’cognitive capabilities(Piemontese,2017)(Figure 1). | Leonardo Brunetti Antonio Laghezza Fulvio Loiodice Paolo Tortorella Luca Piemontese | 2020 | Neural Regeneration Research2020，15，1： | 5 |
| 3 | 美金刚联合盐酸多奈哌齐治疗阿尔茨海默症患者疗效观察显示文摘目的:探讨美金刚联合盐酸多奈哌齐对阿尔茨海默患者认知功能与精神症状的临床疗效。方法:选择阿尔茨海默症患者101例,随机分为观察组(n=51)和对照组(n=50)。对照组采用盐酸多奈哌齐治疗,观察组在对照组基础上联合美金刚治疗,比较2组患者治疗12周后的总有效率与治疗前后的简易智能状态量表(MMSE)评分、阿尔茨海默症行为病理评定量表(BEHAVE-AD)评分。结果:观察组治疗12周后总有效率(96.08%)高于对照组(78.00%)(P<0.05);治疗12周后,2组患者MMSE评分比治疗前高,且观察组MMSE评分[(26.42±2.98)分]高于对照组[(22.42±1.12)分](P<0.05);治疗12周后,2组患者BEHAVE-AD评分比治疗前低,且观察组的BEHAVE-AD评分[(3.42±1.58)分]比对照组[(5.42±0.32)分]低(P<0.05)。结论:美金刚联合盐酸多奈哌齐治疗阿尔茨海默症的临床效果显著,能有效改善患者认知功能与精神症状。 | 王亚军 | 2019 | 长治医学院学报2019，33，3： | 3 |
| 4 | 3,6-二取代三唑并噻二唑衍生物的合成及其对细胞分裂周期25B磷酸酶和蛋白酪氨酸磷酸酶1B抑制活性评价显示文摘合成出了一系列含苯并咪唑/芳氧甲基骨架的3,6-二取代三唑并噻二唑衍生物3a^3l,其结构经傅里叶变换红外光谱仪(FT-IR)、核磁共振波谱仪(NMR)和元素分析得以确认。评价了它们对细胞分裂周期25B磷酸酶(Cdc25B)/蛋白酪氨酸磷酸酶1B(PTP1B)的抑制活性,讨论了构效关系。生物活性测试结果显示,化合物3a对Cdc25B和PTP1B的抑制活性最高,其半数抑制浓度(IC 50)值分别为(0.46±0.02)μg/mL和(1.77±0.40)μg/mL。所得研究结果为开发新型Cdc25B/PTP1B抑制剂提供了参考依据。 | 李英俊 杨鸿境 曹欣 高立信 靳焜 盛丽 刘季红 刘雪洁 李佳 | 2020 | 应用化学2020，37，9： | 2 |
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