新型含肉桂酸片段胆固醇酯衍生物的半合成及生物活性。
Semisynthesis and Pesticidal Activities of Novel Cholesterol Ester Derivatives Containing Cinnamic Acid-like Fragments.
机构信息
College of Plant Protection, Northwest A & F University, Xianyang 712100, China.
Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province, College of Life Science, Huzhou University, Huzhou 313000, China.
出版信息
Molecules. 2022 Dec 2;27(23):8437. doi: 10.3390/molecules27238437.
Due to the extensive use of agrochemicals resulting in the emergence of pesticide resistance and ecological environment problems, the research and development of new alternatives for crop protection is highly desirable. In order to discover potent natural product-based insecticide candidates, a series of new cholesterol ester derivatives containing cinnamic acid-like fragments at the C-7 position were synthesized. Some derivatives showed potent pesticidal activities. Against Walker, compounds , , , and showed 2.1-2.4-fold growth-inhibitory activity of the precursor cholesterol. Against Linnaeus, compounds , , and exhibited 1.9-2.1-fold insecticidal activity of cholesterol. These results will pave the way for the future synthesis of cholesterol-based derivatives as agrochemicals.
由于农用化学品的广泛使用导致了抗药性和生态环境问题的出现，因此非常需要研究和开发新的作物保护替代品。为了发现有效的基于天然产物的杀虫剂候选物，我们合成了一系列在 C-7 位含有肉桂酸样片段的新型胆固醇酯衍生物。一些衍生物表现出很强的杀虫活性。对 Walker，化合物 、 、 、 和 显示出比胆固醇前体高出 2.1-2.4 倍的生长抑制活性。对 Linnaeus，化合物 、 、 和 表现出比胆固醇高出 1.9-2.1 倍的杀虫活性。这些结果为未来合成基于胆固醇的衍生物作为农用化学品铺平了道路。
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