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作 者:吴锦明[1] 沈爱宝[1] 郁伟 范崇光[1] 李英[3]
机构地区:[1]南通大学化学化工学院,江苏南通226007 [2]南通市蔬菜研究所,江苏南通226007 [3]中国科学院上海药物研究所,上海201203
出 处:《农药》2010年第4期303-305,共3页Agrochemicals
基 金:南通市科技局工程技术研究中心项目(D2010;D2001008)
摘 要:以二氢青蒿素为原料合成了10种双二氢青蒿素醚和5种单二氢青蒿素醚,用常规的非选择性叶碟法测定了质量浓度为1.0g/L的合成化合物、青蒿素和二氢青蒿素对菜青虫的生物活性。结果表明:双醚对菜青虫的拒食活性最为显著,处理后24、48h的拒食率分别为85.4%~96.9%和90.9%~98.6%,单醚分别为45.5%~60.6%和50.9%~68.2%,二氢青蒿素为36.6%和42.4%,青蒿素为40.1%和47.0%;双醚同样具有较高的杀虫活性,其处理后96h的校正死亡率为72.7%~95.5%,单醚为45.4%~54.6%,二氢青蒿素为49.9%,青蒿素的杀虫活性不显著。结合活性数据,初步讨论了青蒿素衍生物的构效关系。Ten bisdihydroartemisinin ethers and five monodihydroartemisinin ethers were prepared from dihydroartemisinin. The bioactivities of the synthetic componds, artemisinin and dihydroartemisinin against Pieris rapae larvae were examined by using the conventional no-choice leaf-disk method at 1.0 g/L. The result showed the bis-ethers exhibited higher antifeedant activity, their antifeedant rates were 85.4-96.9% and 90.9-98.6% after 24 and 48 h, the mono-ethers were 45.5-60.6% and 50.9-68.2%, dihydroartemisinin was 36.6% and 42.4%, artemisinin was 40.1 and 47.0%. The bis-ethers also exhibited higher insecticidal activity, their rectified mortality rates were 72.7-95.5% after 96 h, the mono-ethers were 45.4-54.6%, dihydroartemisinin was 49.9%, artemisinin was not noticeable. Based on the activity data, the preliminary structure-activity relationship was also discussed.
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