欢迎登录材料期刊网

材料期刊网

高级检索

以甘草次酸(1)为原料,将其11位羰基还原、30位羧基酯化得11-脱氧甘草次酸-30-乙酯(3).再以四氢呋喃为溶剂,N,N′-二环己基碳二亚胺( DCC)/4-二甲基氨基吡啶(DMAP)为偶合剂,选用Fmoc保护氨基酸对11-脱氧甘草次酸-30-乙酯的3位羟基进行酯化,得到11-脱氧甘草次酸-30-乙酯-3位氨基酸酯衍生物 (4a~4d).化合物4a~4d在V(CHCI2)∶V(Et2 NH)=1∶1溶液中脱去Fmoc保护基得到最终产物(5a ~ 5d),产率80%~87%.化合物5a~5d用1H NMR、EI-MS进行了表征.活性实验结果表明,化合物5a~5d对在高浓度二甲基甲酰胺下生长的枯草芽孢杆菌、大肠杆菌和酵母菌具有保护作用.

参考文献

[1] Finney R S H,Tarknoy A L.The Pharmaco Logical Properties of Glycyrrhetinic Acid Hydrogen Succinate(Disodium Salt)[J].J Pharm Pharmacol,1960,12:49-58.
[2] Farina C,Pinza M,Pifferi G.Synthesis and Anti-ulcer Activity of New Derivatives of Glycyrrhctic Oleanlic and Ursolic Acid[J].IL Farmaco,1998,53:22-32.
[3] Shinbata S,Takahashi K,Yano S,et al.Chemical Modification of Glycyrrnetinic Acid in Relation to the Biological Activities[J].Chem Pharm Bull,1987,35(5):1910-1918.
[4] Glinskii G.Synthetic Glycoamines and Methods for Their Use that Affect Cell Adhesion,Inhibit Cancer Cell Metastasis,and Induce Apoptosis:US,5864024[P],1999-01-26.
[5] Glinskii G.Synthetic Glycoamines that Promote or Inhibit Cell Adhesion:US,5629412[P],1997-05-13.
[6] Schwarz S,Csuk R.Synthesis and Antitumour Activity of Glycyrrhetinic Acid Derivatives[J].Bioorg Med Chem,2010,(18):7458-7474.
[7] YANG Xiaohui,LIU Lijun,REN Binbin,et al.Synthesis and Anti-inflammatory Activeity of 3-Esterified Derivatives of Glycyrrhetinic Acid[J].West Chinese J Pharm Sci,2009,24(3):221-223(in Chinese).杨晓辉,刘利军,任彬彬,等.甘草次酸3-位酯类衍生物的合成及其抗炎活性的研究[J].华西药学杂志,2009,24(3):221-223.
[8] Yon J P,Wang J W,Aisa H A,et al.Synthesis of Glycyrrhetic Acid Derivatives[J].Chem Nat Compd,2008,44(2):194-196.
[9] NI Xuewen,WU Moucheng.Study on Isolation,Identification and the Antibacterial Activity of Ginkgolic Acids[J].Food Sci Technol,2004,25(9):59-63(in Chinese).倪学文,吴谋成.银杏酚酸的分离鉴定及其抗菌活性研究[J].食品科学,2004,25(9):59-63.
上一张 下一张
上一张 下一张
计量
  • 下载量()
  • 访问量()
文章评分
  • 您的评分:
  • 1
    0%
  • 2
    0%
  • 3
    0%
  • 4
    0%
  • 5
    0%