新型11-脱氧甘草次酸-30-酰胺衍生物的研究

目的合成新型的11-脱氧甘草次酸衍生物,寻找抗炎活性高的药物。方法用甘草次酸还原制得11-脱氧甘草次酸,再和R取代的苯基异唑衍生物偶联,合成了一系列新型11-脱氧甘草次酸-30-酰胺衍生物,用IR、1H-NM R1、3C-NM R、M S等分析方法进行结构确证,以苯甲酸引起的小鼠耳肿模型和醋酸引起的小鼠腹膜炎模型评价了抗炎活性。结果IR1、H-NM R1、3C-NM R、M S等数据表明这些化合物结构正确。其中Ⅰ、Ⅲ、Ⅴ和Ⅶ化合物具有明显的抗炎活性,某些甘草次酸-30-酰胺衍生物差异有统计学意义。结论合成的系列新化合物结构正确,具有明显的抗炎活性。

Novel 11-deoxylglycyrrhetinic acid-30-acylam idederivatives

Objective To synthesize the novel derivatives of 11-deoxyl glycyrrhetinic acid with high anti-inflammatory activities.Methods 11-Deoxylglycyrrhetinic acid was obtained by deoxidizing glycyrrhetinic acid with Zn(Hg)/HCl,and then a series of 11-deoxylglycyrrhetinic acid 30 acylamide derivatives were synthesized by coupling with R-Ar-isoxazole-methylamine.And the synthesized compounds were confirmed by the methods of IR,(()~1H-NMR),(()~(13)C-NMR),and MS.Two models were used to evaluate the preliminary anti-inflammatory activity of the compounds.Results The structures of all the new compound were identified by the spectra of IR,(()~1H-NMR),(()~(13)C-NMR),and MS.The compound 1,3,5 and 7 were proven to have a significant anti-inflammatory activity.Conclusion Some 30-acylamide derivatives of glycyrrhetinic acid have significant anti-inflammatory activities.