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.
Export Options
About this article
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 |
![](/images/wayfinder.jpg)
- Author Guidelines
- Bentham Author Support Services (BASS)
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Neuroprotective Gene Therapy for Parkinson’s Disease
Current Gene Therapy Disease Modifying Drugs in Multiple Sclerosis: Mechanisms of Action and New Drugs in the Horizon
CNS & Neurological Disorders - Drug Targets Mechanisms of HIV-1 Tat Neurotoxicity via CDK5 Translocation and Hyper-Activation: Role in HIV-Associated Neurocognitive Disorders
Current HIV Research Viral Inactivation Based on Inhibition of Membrane Fusion: Understanding the Role of Histidine Protonation to Develop New Viral Vaccines
Protein & Peptide Letters The Potential for Genetically Altered Microglia to Influence Glioma Treatment
CNS & Neurological Disorders - Drug Targets Therapeutic Targets in Respiratory Viral Infections
Current Medicinal Chemistry The Role of Natural Products in the Discovery of New Drug Candidates for the Treatment of Neurodegenerative Disorders I: Parkinsons Disease
CNS & Neurological Disorders - Drug Targets Current Concepts on Selected Plant Secondary Metabolites With Promising Inhibitory Effects Against Enzymes Linked to Alzheimer’s Disease
Current Medicinal Chemistry Dichotomous Life of DNA Binding High Mobility Group Box1 Protein in Human Health and Disease
Current Protein & Peptide Science Internal Ribosome Entry Site Elements in Eukaryotic Genomes
Current Genomics Possible Impact of Microglial Cells and the Monocyte-Macrophage System on Suicidal Behavior
CNS & Neurological Disorders - Drug Targets Chemical and Genetic Engineering Strategies to Improve the Potency of Pharmaceutical Proteins and Enzymes
Current Medicinal Chemistry Successful Combination of Sequential Gene Therapy and Rescue Allo-HSCT in Two Children with X-CGD - Importance of Timing
Current Gene Therapy Neurological Aspects of Medical Use of Cannabidiol
CNS & Neurological Disorders - Drug Targets Detection of the M. pneumonia in Synovial Fluid of Children with Negative Culture Arthritis: A Cross Sectional Study in Tehran, Iran
Infectious Disorders - Drug Targets CCR2 Antagonists
Current Topics in Medicinal Chemistry Prevalence of Toxoplasma Encephalitis in AIDS Patients Treated with Didanosine Hospitalised in a French Infectious Service
Current HIV Research Behcets Syndrome: Literature Review
Current Rheumatology Reviews Neuroglobin and Estrogen Receptors: A New Pathway of Cell Survival and Cell Death Balance
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) ATP-Binding Cassette Transporters in Inflammatory Brain Disease
Current Pharmaceutical Design