IR@PKUHSC  > 北京大学药学院  > 化学生物学系
学科主题药学
Design, Synthesis, and Biological Evaluation of (E)-3,4-Dihydroxystyryl Aralkyl Sulfones and Sulfoxides as Novel Multifunctional Neuroprotective Agents
Ning, Xianling1; Guo, Ying1; Wang, Xiaowei1; Ma, Xiaoyan1; Tian, Chao1; Shi, Xueqi1; Zhu, Renzong1; Cheng, Can4; Du, Yansheng5; Ma, Zhizhong3; Zhang, Zhili1; Liu, Junyi1,2
刊名JOURNAL OF MEDICINAL CHEMISTRY
2014-05-22
DOI10.1021/jm500258v
57期:10页:4302-4312
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]ACID PHENETHYL ESTER ; FACTOR-KAPPA-B ; ARTIFICIAL MEMBRANE ; 6-HYDROXYDOPAMINE-INDUCED NEUROTOXICITY ; NEURODEGENERATIVE DISEASES ; ANTIOXIDANT PROPERTIES ; ALZHEIMERS-DISEASE ; HYDROGEN-PEROXIDE ; OXIDATIVE STRESS ; CELLS
英文摘要

Novel (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides were designed and synthesized as new analogues of 1, which showed interesting multifunctional neuroprotective effects, including antioxidative and antineuroinflammatory properties. Specifically, target compounds display excellent potency in scavenging reactive free radicals and demonstrate potent effects against various kinds of toxicities, including H2O2, 6-hydroxydopamine, and lipopolysaccharide in different types of neuronal cells. The antioxidative properties of the target compounds are more potent than that of 1, and the antineuroinflammatory properties are less strong than that of 1. According to the parallel artificial membrane permeation assay for the blood brain barrier, target compounds possess greater blood brain barrier (BBB) permeability than 1. In short, due to improvement of the antioxidative effect, stability, and BBB permeability, (E)-3,4-dihydroxystyryl aralkyl sulfones and sulfoxides can thus be considered as potential multifunctional neuroprotective agents and serve as new lead candidates in the treatment of neurodegenerative diseases.

语种英语
WOS记录号WOS:000336510100028
Citation statistics
Cited Times:21[WOS]   [WOS Record]     [Related Records in WOS]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/60499
Collection北京大学药学院_化学生物学系
北京大学基础医学院
北京大学药学院
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Peking Univ, Sch Basic Med Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
3.Peking Univ, Sch Basic Med Sci, Dept Integrat Chinese & Western Med, Beijing 100191, Peoples R China
4.Jiangxi Univ Tradit Chinese Med, Dept Pharmaceut Chem, Nanchang 330004, Peoples R China
5.Indiana Univ Sch Med, Dept Neurol, Indianapolis, IN 46202 USA
Recommended Citation
GB/T 7714
Ning, Xianling,Guo, Ying,Wang, Xiaowei,et al. Design, Synthesis, and Biological Evaluation of (E)-3,4-Dihydroxystyryl Aralkyl Sulfones and Sulfoxides as Novel Multifunctional Neuroprotective Agents[J]. JOURNAL OF MEDICINAL CHEMISTRY,2014,57(10):4302-4312.
APA Ning, Xianling.,Guo, Ying.,Wang, Xiaowei.,Ma, Xiaoyan.,Tian, Chao.,...&Liu, Junyi.(2014).Design, Synthesis, and Biological Evaluation of (E)-3,4-Dihydroxystyryl Aralkyl Sulfones and Sulfoxides as Novel Multifunctional Neuroprotective Agents.JOURNAL OF MEDICINAL CHEMISTRY,57(10),4302-4312.
MLA Ning, Xianling,et al."Design, Synthesis, and Biological Evaluation of (E)-3,4-Dihydroxystyryl Aralkyl Sulfones and Sulfoxides as Novel Multifunctional Neuroprotective Agents".JOURNAL OF MEDICINAL CHEMISTRY 57.10(2014):4302-4312.
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