Copper-catalyzed Tandem Trifluoromethylation/ Cyclization of Internal Alkynes
文献类型：期刊论文
| 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 |
| 刊名 | Org. Chem. Front.
 |
| 出版日期 | 2014 |
| 卷号 | 1页码:1280-1284 |
| 其他题名 | 铜催化下中间炔的串联三氟甲基化/环化反应 |
| 通讯作者 | 林锦鸿 ; 肖吉昌 |
| 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. |
| 学科主题 | 氟化学; 金属有机化学 |
| 原文出处 | http://dx.doi.org/10.1039/c4qo00240g |
| 语种 | 英语 |
| 源URL | [http://ir.sioc.ac.cn/handle/331003/38828]  |
| 专题 | 上海有机化学研究所_中科院有机氟化学重点实验室 |
| 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 |
| 推荐引用方式 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. |
入库方式： OAI收割
来源：上海有机化学研究所
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