Wu Rui, Zhu Cong, Du Xiu-Jiang, Xiong Li-Xia, Yu Shu-Jing, Liu Xing-Hai, Li Zheng-Ming, Zhao Wei-Guang
State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.
Chem Cent J. 2012 Sep 11;6(1):99. doi: 10.1186/1752-153X-6-99.
Culex is an important mosquito as vectors for the transmission of serious diseases, such as filariasis, West Nile virus, dengue, yellow fever, chikungunya and other encephalitides. Nearly one billion people in the developing countries are at risk. In order to discover new bioactive molecules and pesticides acting on mosquito, we designed active amide structure and synthesized a series of novel diamide derivatives.
A series of novel diamide derivatives were designed and synthesized. Their structures were characterized by 1 H NMR, FTIR and HRMS. The single crystal structure of compound 6n was determined to further elucidate the structure. Biological activities of these compounds were tested. Most of them exhibited higher mosquito larvicidal activity. Especially compound 6r displayed relatively good activity to reach 70% at 2 μg/mL.
A practical synthetic route to amide derivatives by the reaction of amide with another acid is presented. This study suggests that the diamide derivatives exhibited good effective against mosquito.
库蚊是一种重要的蚊子，作为传播严重疾病的媒介，如丝虫病、西尼罗河病毒、登革热、黄热病、基孔肯雅热和其他脑炎。发展中国家近十亿人面临风险。为了发现作用于蚊子的新生物活性分子和杀虫剂，我们设计了活性酰胺结构并合成了一系列新型二酰胺衍生物。
设计并合成了一系列新型二酰胺衍生物。通过1H NMR、FTIR和HRMS对其结构进行了表征。测定了化合物6n的单晶结构以进一步阐明结构。测试了这些化合物的生物活性。它们中的大多数表现出较高的杀蚊幼虫活性。特别是化合物6r表现出相对较好的活性，在2μg/mL时达到70%。
提出了一种通过酰胺与另一种酸反应合成酰胺衍生物的实用路线。本研究表明，二酰胺衍生物对蚊子表现出良好的效果。
