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学科主题: 药学
题名:
Design, Synthesis, and Biological Evaluation of (E)-3,4-Dihydroxystyryl Aralkyl Sulfones and Sulfoxides as Novel Multifunctional Neuroprotective Agents
作者: 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
发表日期: 2014-05-22
DOI: 10.1021/jm500258v
卷: 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
所属项目编号: 20972011 ; 21042009 ; 21172014 ; 2009ZX09301-010
项目资助者: National Natural Science Foundation of China ; Ministry of Science and Technology of China
WOS记录号: WOS:000336510100028
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/60499
Appears in Collections:北京大学药学院_化学生物学系_期刊论文

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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:
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.
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