虞佩琳, 陈一心, 李英, 嵇汝运. 青蒿素类似物的研究 Ⅳ.含卤素、氮、硫等杂原子的青蒿素衍生物的合成J. 药学学报, 1985, 20(5): 357-365.
引用本文: 虞佩琳, 陈一心, 李英, 嵇汝运. 青蒿素类似物的研究 Ⅳ.含卤素、氮、硫等杂原子的青蒿素衍生物的合成J. 药学学报, 1985, 20(5): 357-365.
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YU Pei-Lin, CHEN Yi-Xin, LI Ying , JI Ru-Yun, . STUDIES ON ANALOGS OF QINGHAOSU (ARTEMISININE,ARTEANNUIN) IV. SYNTHESIS OF DERIVATIVES OF QINGHAOSU CONTAINING HALOGEN,NITROGEN AND SULFUR HETEROATOMSJ. Acta Pharmaceutica Sinica, 1985, 20(5): 357-365.
Citation: YU Pei-Lin, CHEN Yi-Xin, LI Ying , JI Ru-Yun, . STUDIES ON ANALOGS OF QINGHAOSU (ARTEMISININE,ARTEANNUIN) IV. SYNTHESIS OF DERIVATIVES OF QINGHAOSU CONTAINING HALOGEN,NITROGEN AND SULFUR HETEROATOMSJ. Acta Pharmaceutica Sinica, 1985, 20(5): 357-365.
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青蒿素类似物的研究 Ⅳ.含卤素、氮、硫等杂原子的青蒿素衍生物的合成

STUDIES ON ANALOGS OF QINGHAOSU (ARTEMISININE,ARTEANNUIN) IV. SYNTHESIS OF DERIVATIVES OF QINGHAOSU CONTAINING HALOGEN,NITROGEN AND SULFUR HETEROATOMS

    摘要
  • 摘要: 为增强双氢青蒿素酯和醚类衍生物的抗疟作用,我们合成了42个侧链上带有卤素、氮或硫取代的双氢青蒿素酯和醚类化合物。抗疟筛选表明,多数化合物的活性高于青蒿素,但并未超过相应的无杂原子取代的衍生物,唯双氢青蒿素的问-三氟甲基苯甲酸酯(17)的抗疟活性为间-甲基苯甲酸酯的4倍,化合物(17)和(6)为青蒿素的10倍。

     

    Abstract: In order to search for novel potent antimalarials, a series of ethers and esters of dihydroqinghaosu with halogen, nitrogen and sulfur heteroatoms substisuted in their side chain was prepared. However, these compounds did not show advantage over the corresponding unsubstituted derivatives except compound (17) which was found to be four times as active as m-methylbenzoic ester of dihydroqinghaosu. Compound(17)and(6)were ten times as active as qinghaosu against plasmodium berghei in mice.

     

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