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.
Keywords: 1, 2, 3-triazole, acetamide, click synthesis, larvicidal activity.
Combinatorial Chemistry & High Throughput Screening
Title:Larvicidal Activity and Click Synthesis of 2-Alkoxyl-2-(1,2,3-Triazole-1- yl)Acetamide Library
Volume: 16 Issue: 6
Author(s): Na-Na Su, Li-Xia Xiong, Shu-Jing Yu, Xiao Zhang, Can Cui, Zheng-Ming Li and Wei-Guang Zhao
Affiliation:
Keywords: 1, 2, 3-triazole, acetamide, click synthesis, larvicidal activity.
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.
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Cite this article as:
Su Na-Na, Xiong Li-Xia, Yu Shu-Jing, Zhang Xiao, Cui Can, Li Zheng-Ming and Zhao Wei-Guang, Larvicidal Activity and Click Synthesis of 2-Alkoxyl-2-(1,2,3-Triazole-1- yl)Acetamide Library, Combinatorial Chemistry & High Throughput Screening 2013; 16 (6) . https://dx.doi.org/10.2174/1386207311316060009
DOI https://dx.doi.org/10.2174/1386207311316060009 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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