SIOC OpenIR  > 中科院有机氟化学重点实验室
Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes
其他题名铜催化下中间炔的串联三氟甲基化/环化反应
Ji YL(季云龙)1; Lin JH(林锦鸿)1; Xiao JC(肖吉昌)1; Gu YC(顾玉诚)1
2014
发表期刊Org. Chem. Front.
卷号1页码:1280-1284
摘要Glial activation-mediated neuroinflammation plays a pivotal role in the process of several neuroinflammatory diseases including stroke, Alzheimer's diseases, Parkinson's diseases, multiple sclerosis and ischemia. Inhibition of microglial activation may ameliorate neuronal degeneration under the inflammatory conditions. In the present study, a number of 5 alpha-cholestan-6-one derivatives were prepared and the anti-inflammatory effects of these compounds were evaluated in LPS-stimulated BV-2 microglia cells. Those derivatives were synthesized from readily available hyodeoxycholic acid (1). Among the tested compounds, several analogs (16-18, 25, 35, 38) exhibited potent inhibitory activities on nitric oxide production with no or weak cell toxicity. Compound 16 also significantly suppressed the expression of TNF-alpha, interleukin (IL)-1 beta, cyclooxygenase (COX-2) as well as inducible nitric oxide synthase (iNOS) in LPS-stimulated BV-2 microglia cells. In addition, compound 16 markedly reduced infarction volume in a focal ischemic mice model. (C) 2013 Elsevier Ltd. All rights reserved.
学科领域氟化学 ; 金属有机化学
DOI10.1039/c4qo00240g
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语种英语
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被引频次:21[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.sioc.ac.cn/handle/331003/38828
专题中科院有机氟化学重点实验室
通讯作者Lin JH(林锦鸿); Xiao JC(肖吉昌)
作者单位1.中科院上海有机化学研究所
2.英国先正达公司
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GB/T 7714
Ji YL,Lin JH,Xiao JC,et al. Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes[J]. Org. Chem. Front.,2014,1:1280-1284.
APA 季云龙,林锦鸿,肖吉昌,&顾玉诚.(2014).Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes.Org. Chem. Front.,1,1280-1284.
MLA 季云龙,et al."Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes".Org. Chem. Front. 1(2014):1280-1284.
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