鹿蹄草素酯类衍生物的合成及抗菌活性研究(1)
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[摘要] 目的 为了延长鹿蹄草素作用时间，减少给药频率，合成鹿蹄草素酯类衍生物，通过实验筛选活性分子，以便进一步开发利用鹿蹄草素。 方法 利用前药原理，将鹿蹄草素两个酚羟基酰化保护，通过不同的方法合成5个鹿蹄草素酰基化合物，用大肠杆菌和金黄色葡萄球菌致小鼠死亡实验，考察5个鹿蹄草素酰基化合物的药理作用。 结果 通过IR、1H-NMR、13C-NMR、ESI-MS对酰基化合物进行了结构鉴定，分别为双乙酰化鹿蹄草素、双丙酰化鹿蹄草素、双苯甲酰化鹿蹄草素、双烟酰化鹿蹄草素、双乙酰水杨酰化鹿蹄草素。体内抗菌实验显示对金黄色葡萄球菌、大肠杆菌所引起的感染小鼠存活率明显提高(P<0.01)，酰基衍生物的抑菌效果比鹿蹄草素明显。 结论 合成的五个鹿蹄草素酰基化合物有很好的体内抗菌活性，有进一步研究开发的价值。
[关键词] 鹿蹄草素；衍生物；结构修饰；活性筛选
[中图分类号] TQ463.4 [文献标识码] A [文章编号] 1673-7210(2012)01(b)-019-03
Study on synthesis of Pyrolin ester derivatives and antibacterial activity
HE Yong1 LI Jiaming2
1.Department of Pharmacy, the People′s Hospital of Chizhou in Anhui Province, Chizhou 247000, China; 2.College of Pharmacy, Anhui College of Traditional Chinese Medicine in Anhui Province, Hefei 230031, China
[Abstract] Objective To prolong the action times and reduce the administration times of Pyrolin. Then to synthesis ester derivatives of Pyrolin and screen the activity molecular with pharmacological experiment. Methods Five Pyrolin-acyl derivatives were prepared from Pyrolin, through the different methods of using before medicine principle to protect the two phenolic hydroxyl acylation of Pyrolin. Then the pharmacological function of five Pyrolin-acyl derivatives were investigated by death experiment of rats induced by staphylococcus aureus and escherichia coli. Results The structures of the target compounds were identified by IR, 1H-NMR, 13C-NMR and ESI-Ms, which were diacetyl-Pyrolin, dipropionyl-Pyrolin, dibenzoyl-Pyrolin, dinicotinate-Pyrolin, diacetyl-salicylic-Pyrolin. The antibacerial experiments in vivo showed the target compounds signicantly increased the survival rates of rats which were infected with escherichia coli and staphylococcus aureus (P<0.01). The antibacterial effect of the target compounds were better than Pyrolin. Conclusion Five synthesized target compounds have good antibacterial activities in vivo, and they are valuable to further study.
[Key words] Pyrolin; Derivatives; Structure modification; Activity screening ......
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