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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents
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Synthesis, structure-activity relationships and biological evaluation of dehydroandrographolide and andrographolide derivatives as novel anti-hepatitis B virus agents

机译：脱氢天文苷与脱羟化物衍生物作为新型抗乙型肝炎病毒剂的合成，结构 - 活性关系和生物学评价

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摘要

Dehydroandrographolide and andrographolide, two natural diterpenoids isolated from Andrographis paniculata possessed activity against HBV DNA replication with IC50 values of 22.58 and 54.07 μM and low SI values of 8.7 and 3.7 in our random assay. Consequently, 48 derivatives of dehydroandrographolide and andrographolide were synthesized and evaluated for their anti-HBV properties to yield a series of active derivatives with lower cytotoxicity, including 14 derivatives against HBsAg secretion, 19 derivatives against HBeAg secretion and 38 derivatives against HBV DNA replication. Interestingly, compound 4e could inhibit not only HBsAg and HBeAg secretions but also HBV DNA replication with SI values of 20.3, 125.0 and 104.9. Furthermore, the most active compound 2c with SI value higher than 165.1 inhibiting HBV DNA replication was revealed with the optimal log P value of 1.78 and log D values. Structure-activity relationships (SARs) of the derivatives were disclosed for guiding the future research toward the discovery of new anti-HBV drugs.
机译：从Andrographis Paniculata分离的两种自然二萜类化合物和Andrographolide，在我们的随机测定中具有22.58和54.07μm的IC 50值，具有22.58和54.07μm的HBV DNA复制的活性。因此，合成并评估了48种脱氢天文化剂和andrographolide的抗HBV性质，得到一系列具有较低细胞毒性的活性衍生物，其中包含14个针对HBSAG分泌的衍生物，其抗HBEAg分泌的衍生物和针对HBV DNA复制的38个衍生物。有趣的是，化合物4e不仅可以抑制HBsAg和HBeAg分泌物，还可以抑制HBV DNA复制，Si值为20.3,125.0和104.9。此外，具有高于165.1的抑制HBV DNA复制的最佳活性化合物2C，并用1.78的最佳日志P值和log D值揭示了抑制HBV DNA复制。透露了衍生品的结构 - 活动关系（SARS），用于指导未来的研究发现新的抗HBV药物。

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    ChenH.; MaY.-B.; HuangX.-Y.; GengC.-A.; ZhaoY.; WangL.-J.; GuoR.-H.; LiangW.-J.; ZhangX.-M.; ChenJ.-J.;

  • 作者单位

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

    State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of;

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  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    Anti-HBV activity; Dehydroandrographolide and andrographolide derivatives; Octanol-water partition coefficients; Structure-activity relationships;

    机译：抗HBV活性;脱氢型甲基衍生物;辛醇 - 水分配系数;结构 - 活动关系;

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