Larvicidal activity and click synthesis of 2-alkoxyl-2-(1,2,3-triazole-1- yl)acetamide library.
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 2 µg.mL⁻¹ were 100% and 73% respectively.
State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center-Tianjin, Nankai University, Tianjin 300071, China.
Na-Na
NN
Su
Li-Xia
LX
Xiong
Shu-Jing
SJ
Yu
Xiao
X
Zhang
Can
C
Cui
Zheng-Ming
ZM
Li
Wei-Guang
WG
Zhao
D000081:Acetamides / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D002384:Catalysis; D002606:Charcoal / Q000737:chemistry; D057930:Click Chemistry; D003300:Copper / Q000737:chemistry; D009033:Culicidae / Q000187:drug effects* / Q000254:growth & development*; D007306:Insecticides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007814:Larva / Q000187:drug effects; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D000081:Acetamides; D007306:Insecticides; D054852:Small Molecule Libraries; D014230:Triazoles; D002606:Charcoal; D003300:Copper