Liu Xing-Hai, Wang Qiao, Sun Zhao-Hui, Wedge David E, Becnel James J, Estep Alden S, Tan Cheng-Xia, Weng Jian-Quan
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, China.
USDA-ARS, Natural Products Utilization Research Unit, University, MS, USA.
Pest Manag Sci. 2017 May;73(5):953-959. doi: 10.1002/ps.4370. Epub 2016 Sep 1.
Aedes aegypti is a major mosquito vector for the transmission of serious diseases, especially dengue and yellow fever. More than 1 billion people in developing countries are at risk. The widespread and continual use of pesticides can lead to resistant mosquitoes. In order to maintain mosquito control gains, it is critical to develop and evaluate novel bioactive molecules that differ in mode of action from currently used products.
A series of novel pyrimidine derivatives were designed and synthesized. Their structures were elucidated by proton nuclear magnetic resonance spectroscopy and high-resolution mass spectrometry. The biological activities of these compounds were tested against Ae. aegypti. Many of them exhibited insecticidal activity against adult and larval mosquitoes. Compound 4d displayed relatively good activity to reach 70% mortality at 2 µg mL . Furthermore, density functional theory calculations were established to study the structure-activity relationship of these novel compounds.
A practical synthetic route for pyrimidine derivatives is presented. This study suggests that these pyrimidine derivatives exhibit some activity against the yellow fever mosquito and, with further structure modification, could be novel lead compounds for the development of insecticides against mosquitoes. © 2016 Society of Chemical Industry.
埃及伊蚊是传播严重疾病（尤其是登革热和黄热病）的主要蚊虫媒介。发展中国家超过10亿人面临风险。农药的广泛持续使用会导致蚊虫产生抗性。为了保持蚊虫控制成果，开发和评估作用方式与现有产品不同的新型生物活性分子至关重要。
设计并合成了一系列新型嘧啶衍生物。通过质子核磁共振光谱和高分辨率质谱对其结构进行了阐明。测试了这些化合物对埃及伊蚊的生物活性。其中许多对成年和幼虫蚊虫表现出杀虫活性。化合物4d表现出相对较好的活性，在2 µg/mL时死亡率达到70%。此外，建立了密度泛函理论计算以研究这些新型化合物的构效关系。
提出了一种实用的嘧啶衍生物合成路线。本研究表明这些嘧啶衍生物对黄热病蚊虫表现出一定活性，通过进一步的结构修饰，可能成为开发抗蚊杀虫剂的新型先导化合物。© 2016化学工业协会。
