Larvicidal Activity and Click Synthesis of 2-Alkoxyl-2-(1,2,3-Triazole-1- yl)Acetamide Library

E-ISSN： 1875-5402|16|6|484-493

ISSN： 1386-2073

Source： Combinatorial Chemistry & High Throughput Screening, Vol.16, Iss.6, 2013-07, pp. : 484-493

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Abstract

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.