王晓晶, 杨淬, 王兴红, 黄超. 剑叶龙血素A衍生物的合成及其镇痛活性研究[J]. 云南大学学报(自然科学版), 2018, 40(4): 748-754. doi: 10.7540/j.ynu.20180055
引用本文: 王晓晶, 杨淬, 王兴红, 黄超. 剑叶龙血素A衍生物的合成及其镇痛活性研究[J]. 云南大学学报(自然科学版), 2018, 40(4): 748-754. doi: 10.7540/j.ynu.20180055
WANG Xiao-jing, YANG Cui, WANG Xing-hong, HUANG Chao. Synthesis and analgesic activity evaluation of cochinchinenin A derivatives[J]. Journal of Yunnan University: Natural Sciences Edition, 2018, 40(4): 748-754. DOI: 10.7540/j.ynu.20180055
Citation: WANG Xiao-jing, YANG Cui, WANG Xing-hong, HUANG Chao. Synthesis and analgesic activity evaluation of cochinchinenin A derivatives[J]. Journal of Yunnan University: Natural Sciences Edition, 2018, 40(4): 748-754. DOI: 10.7540/j.ynu.20180055

剑叶龙血素A衍生物的合成及其镇痛活性研究

Synthesis and analgesic activity evaluation of cochinchinenin A derivatives

  • 摘要: 以苯乙酮衍生物及2,6-二甲氧基苯甲醛为起始原料,经2步高效合成了20个剑叶龙血素A衍生物,其中12个为新化合物,化合物结构经1H NMR,13C NMR,IR及HRMS进行确证.在此基础上,以盐酸曲马多为阳性对照组,经扭体法实验对所合成的化合物进行镇痛活性研究,初步活性结果表明,化合物4d1(8.33±1.45/次,13.00±4.16/次,8.67±3.71/次),5e(5.67±2.40/次,12.67±1.45/次,13.00±5.68/次)与阳性对照组(6.67±1.20/次)的活性相当.以龙血竭中剑叶龙血素A为母体,合成其衍生物并评价其镇痛活性,为进一步研究龙血竭镇痛活性提供了参考.

     

    Abstract: Based on the structure of cochinchinenin A,twenty conchinchinenin A derivatives were designed and synthesized via two steps reactions of acetophenone derivatives and 2,6-dimethoxybenzaldehyde.The structures of the obtained compounds were characterized by 1H NMR,13C NMR,IR and HRMS.And on this basis,with tramadol hydrochloride as positive control group,the writhing test the analgesic activity of the synthesized compounds was evaluated.The biological results demonstrated that compounds 4d1(8.33±1.45,13.00±4.16,8.67±3.71) and 5e(5.67±2.40,12.67±1.45,13.00±5.68) were commensurate with tramadol hydrochloride (6.67±1.20) in analgesic activity. The studies provide a reference for the further development of Dragon's blood in analgesic activity.

     

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