摘要
目的:对苗药马蹄金的活性成分马蹄金素[N-(N-苯甲酰基-L-苯丙氨酰基)-O-乙酰基-L-苯丙氨醇,MTS]进行结构修饰,以期获得抗乙肝病毒(HBV)活性更好、毒性更低目标分子。方法:以MTS为先导化合物,设计合成一系列含氮杂环取代的MTS衍生物并对其进行抗HBV活性测试。结果:合成了新的MTS衍生物共计6个,经体外活性筛选结果显示有3个衍生物具有抗HBV活性。结论:化合物4b、6b、6c显示较好的抗HBV活性,说明含氮杂环取代的苗药马蹄金的活性成分MTS衍生物值得深入研究。
Objective:To develop new anti-hepatitis B virus(HBV) agents with high anti-HBV activity from Matijin-Su [N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol, MTS], isolated from Miao Ethnomedicine Matijin(Dichondra repens Forst). Methods: A series of MTS derivatives with nitrogen-containing heterocycles were designed, synthesized and evaluated for their anti-HBV activity in HepG2 2.2.15 cells. Results: Six new derivatives of MTS were synthesized and three compounds exhibited anti-HBV activity. Conclusion: Derivative 4 b, 6 b and 6 c have good anti-HBV activity,which means that the MTS derivatives with nitrogen-containing heterocycles are worth of further research.
引文
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