| 马蹄金素类似物的合成及其初步抗HBV活性研究 |
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| 引用本文： | 梁光平,;胡占兴,;杨秀虾,;刘青川,;黄正明,;梁光义,;徐必学. 马蹄金素类似物的合成及其初步抗HBV活性研究[J]. 中南药学, 2014, 0(9): 852-855 |
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| 作者姓名： | 梁光平, 胡占兴, 杨秀虾, 刘青川, 黄正明, 梁光义, 徐必学 |
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| 作者单位： | [1]贵州省中国科学院天然产物化学重点实验室,贵阳550002; [2]贵阳中医学院,贵阳550002; [3]中国人民解放军第三О二医院,北京100039 |
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| 基金项目： | 国家自然科学基金资助项目（No.81360472） |
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| 摘 要： | 目的合成马蹄金素[N-(N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇,MTS]的类似物,以期寻找高效低毒的抗乙肝病毒化合物。方法以L-苯丙氨酸为起始原料,通过磺酰化、酰化、水解、烷基化等反应,合成马蹄金素类似物并对其进行体外抗乙肝病毒活性测试。结果合成了7个具有磺酰胺结构片段的马蹄金素类似物,活性测试结果显示所有的目标产物均有不同程度的抗乙肝病毒活性,有3个化合物在8μg·mL-1的浓度下具有较高的抑制率,分别为2b(41.9%)、2d(61.3%)、3(47.5%)。结论其中2d显示出较强的抗HBV活性,在3.2μg·mL-1时抑制率也有50.9%,具有进一步研究开发的价值。
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| 关 键 词： | 马蹄金素 类似物 合成 抗HBV活性 |
Synthesis and anti-hepatitis B virus activity of Matijin-Su analogues |
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| Affiliation: | LIANG Guang-ping, HU Zhan-xing, YANG Xiu-xia, LIU Qing-chuan, HUANG Zheng-ming, LIANG Guang- yi, XU Bi-xue(1. Key Laboratory of Chemistry for Natural Products, Chinese Academy of Sciences of Guizhou, Guiyang 550002; 2. Guiyang College of Traditional Chinese Medicine, Guiyang 550002; 3. 302 Hos- pital of the PLA, Beijing 100039) |
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| Abstract: | Objective To find new anti-hepatitis B virus （HBV） compounds with high activity and low toxicity from Matijin-Su [N-（N-benzoyl-L-phenylalanyl）-O-acetyl-L-phenylalanol] （MTS）. Methods A series of MTS analogues were synthesized by sulfonamide, acylation, hydrolysis, alkylation reactions and their anti-HBV activity evaluated in HepG2 2.2.15 cells. Results Seven analogues with sulfonamide structure of MTS were synthesized and 3 of these com- pounds exhibited high inhibition rate at 8μg · mL - 12b （41.9%）, 2d （61.3%） and 3 （47.5%）. Conclusion The ana- logues of 2d have potent anti-HBV activity, which shows 50.9% of inhibition rate anti-HBV activity at 3.2 μg ·mL 1 and is worthy of further research. |
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| Keywords: | Matijin-Su analogues synthesis activity of anti-hepatitis B virus |
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