📜1-(4-氟苯基)-2-(4-吡啶基)乙酮置于盐酸,Ammonium Acetate,溶剂黄146,Sodium Nitrite,亚磷酸三乙酯体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 22.5H,反应生成4-(4-氟苯基)-2-(4-羟基苯基)-5-(4-吡啶基)-1H-咪唑 参考文献:Regulation Of Stress-Induced Cytokine Production By Pyridinylimidazoles; Inhibition Of Csbp Kinase 标题:Regulation Of Stress-Induced Cytokine Production By Pyridinylimidazoles; Inhibition Of Csbp Kinase 摘要:Members Of Three Classes Of Pyridinylimidazoles Bind With Varying Affinities To Csbp (P38) Kinase Which Is A Member Of A Stress-Induced Signal Transduction Pathway. Based Upon Sar And Protein Homology Modeling,The Pharmacophore And Three Potential Modes Of Binding To The Enzyme Are Presented. For A Subset Of Pyridinylimidazoles,Binding Is Shown To Correlate With Inhibition Of Csbp Kinase Activity,Whereas No Significant Inhibition Of Pka,Pkc Alpha And Erk Kinase Activity Is Observed. Copyright (C) 1997 Elsevier Science Ltd. Doi:10.1016/s0968-0896(96)00212-X
专利号:US-8557837-B2 优先权日:2010-02-10 标题:Sinomenine derivatives, synthetic methods and uses thereof 发明人:YAO ZHUJUN; SUN BING; LOU YANGTONG; YANG ZHENYU; CHEN AIZHONG; MA ZHAO 权利人:YAO ZHUJUN; SUN BING; LOU YANGTONG; YANG ZHENYU; CHEN AIZHONG; MA ZHAO; SHANGHAI INST ORGANIC CHEM; SHANGHAI INST BIOL SCIENCES 摘要:The invention relates to sinomenine derivatives, methods for their synthesis and their applications. The sinomenine derivatives include oxidation derivatives, and C-10 substituted sinomenine derivatives. Based on the readily oxidizable phenol group on sinomenine structure, using oxidation, oxidative dearomatization, or conjugated addition aromatization, one can introduce C-10 substitutions to synthesize the sinomenine derivatives. The sinomenine derivatives of the invention have the following structures: n n n n n n n n n n Using in vitro TNF-α inhibition assay, the activities of the synthetic compounds are assessed. Results from these assays shown that most compounds have anti-inflammatory effects, and some compounds have better activities than that of sinomenine. These compounds may be used in treating immune diseases such as rheumatoid arthritis (RA).
专利号:CN-101798285-A 优先权日:2010-02-10 标 题:A kind of sinomenine derivative, synthesis method and application thereof
专利号:CN-101798285-B 优先权日:2010-02-10 标 题 :A kind of sinomenine derivative, synthesis method and application thereof
1: Davies SP, Reddy H, Caivano M, Cohen P. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095. 2: Shanware NP, Williams LM, Bowler MJ, Tibbetts RS. Non-specific in vivo inhibition of CK1 by the pyridinyl imidazole p38 inhibitors SB 203580 and SB 202190. BMB Rep. 2009 Mar 31;42(3):142-7. doi: 10.5483/bmbrep.2009.42.3.142. 3: Glover M, Sweeny C, Davis B, O'Shaughnessy KM. A Single Amino Acid Substitution Makes WNK4 Susceptible to SB 203580 and SB 202190. Open Med Chem J. 2010 Sep 3;4:57-61. doi: 10.2174/1874104501004010057.
合成参考文献
参考文献:10.1016/j.toxlet.2011.06.029 摘要:Umannová L, Machala M, Topinka J, Schmuczerová J, Krčmář P, Neča J, Šujanová K, Kozubík A, Vondráček J. Benzo[a]pyrene and tumor necrosis factor-α coordinately increase genotoxic damage and the production of proinflammatory mediators in alveolar epithelial type II cells. Toxicol Lett. 2011 Oct 10;206(2):121–9. doi: 10.1016/j.toxlet.2011.06.029. 参考文献:10.1016/j.cellsig.2011.07.002 摘要:Walters JN, Bickford JS, Beachy DE, Newsom KJ, Herlihy JH, Peck MV, Qiu X, Nick HS. cPLA2α gene activation by IL-1β is dependent on an upstream kinase pathway, enzymatic activation and downstream 15-lipoxygenase activity: A positive feedback loop. Cellular Signalling. 2011 Dec;23(12):1944–51. doi: 10.1016/j.cellsig.2011.07.002.