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

Author(s): Na-Na Su, Li-Xia Xiong, Shu-Jing Yu, Xiao Zhang, Can Cui, Zheng-Ming Li, Wei-Guang Zhao

Journal Name: Combinatorial Chemistry & High Throughput Screening
Accelerated Technologies for Biotechnology, Bioassays, Medicinal Chemistry and Natural Products Research

Volume 16 , Issue 6 , 2013

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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.

Keywords: 1, 2, 3-triazole, acetamide, click synthesis, larvicidal activity.

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Article Details

Year: 2013
Page: [484 - 493]
Pages: 10
DOI: 10.2174/1386207311316060009
Price: $65

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