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学科主题: 氟化学; 金属有机化学
题名: 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
作者: Ji YL(季云龙)1; Lin JH(林锦鸿)1; Xiao JC(肖吉昌)1; Gu YC(顾玉诚)1
通讯作者: 林锦鸿 ; 肖吉昌
刊名: Org. Chem. Front.
发表日期: 2014
DOI: 10.1039/c4qo00240g
卷: 1, 页:1280-1284
英文摘要: 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.
语种: 英语
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/38828
Appears in Collections:中科院有机氟化学重点实验室_期刊论文

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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

Recommended Citation:
Ji YL,Lin JH,Xiao JC,et al. Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes[J]. Org. Chem. Front.,2014,1:1280-1284.
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