Larvicidal Activity and Click Synthesis of 2-Alkoxyl-2-(1,2,3-Triazole-1- yl)Acetamide Library
作者:Na-Na Su、Li-Xia Xiong、Shu-Jing Yu、Xiao Zhang、Can Cui、Zheng-Ming Li、Wei-Guang Zhao
DOI:10.2174/1386207311316060009
日期:2013.4.1
Heterogeneous copper-in-charcoal-catalyzed click synthesis in 96-well polypropylene filter plates is an
efficient method for the rapid generation of sufficient pure 2-alkoxyl-2-(1,2,3-triazole-1-yl) acetamide derivatives library
by simple filtration, which directly assay the products for larvicidal activity against mosquitoes. In this procedure, copper
nanoparticles on charcoal were arrayed into each well on a 96-well plate, reagents were delivered using a pipette gun, and
a constant temperature shaker bath was used to complete the click reaction in 24-72 hours under temperature-controlled
conditions. The results of bioassays indicated that the target compounds possessed excellent larvacidal activities against
mosquitoes. In particular, the larvacidal activities against mosquitoes of compounds 8[2,3] and 8[7,1] at 2µg.mL-1 were
100% and 73%respectively.
异质铜-炭催化点击合成在96孔聚丙烯过滤板中是一种高效的方法,通过简单的过滤,能快速生成足够纯的2-烷氧基-2-(1,2,3-三唑-1-基)乙酰胺衍生物库,并直接对产品进行对蚊子的杀幼活性检测。在此过程中,铜纳米颗粒散布在炭上,分别排列在每个96孔板上,使用移液枪传送试剂,并在恒温摇床中在温度控制条件下在24至72小时内完成点击反应。生物测试结果表明,目标化合物对蚊子具有极佳的杀幼活性。特别是化合物8[2,3]和8[7,1]在2µg.mL-1浓度下对蚊子的杀幼活性分别为100%和73%。