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Research Project: Health-Promoting Bioactives and Biobased Pesticides from Medicinal and Herbal Crops

Location: Natural Products Utilization Research

Title: Synthesis and mosquiticidal activity of novel hydrazone containing pyrimidine derivatives against Aedes aegypti

Author
item SHEN, ZHONG-HUA - Zhejiang University Of Technology
item SUN, ZHAO-HUI - Zhejiang University Of Technology
item Becnel, James
item ESTEP, ALDEN - Zhejiang University Of Technology
item Vacant, Vacant
item TAN, CHENG-XIA - Zhejiang University Of Technology
item WENG, JIAN-QUAN - Zhejiang University Of Technology
item LIU, XING-HAI - Zhejiang University Of Technology

Submitted to: Letters in Drug Design & Discovery
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 12/22/2017
Publication Date: 1/1/2018
Citation: Shen, Z., Sun, Z., Becnel, J.J., Estep, A.S., Wedge, D.E., Tan, C., Weng, J., Liu, X. 2018. Synthesis and mosquiticidal activity of novel hydrazone containing pyrimidine derivatives against Aedes aegypti. Letters in Drug Design & Discovery. 15(9):951-956. doi:10.2174/1570180815666180102141640.
DOI: https://doi.org/10.2174/1570180815666180102141640

Interpretive Summary: Mosquitoes are vectors of pathogens that cause disease in man and animals. New public health pesticides for mosquito control are desperately needed because of resistance issues with the only two classes of chemicals registered for use in integrated mosquito management programs. This paper examines the structures and efficacy of a group of newly synthesized hydrazones for their ability to kill immature and adult stages of the Yellow fever mosquito Aedes aegypti. Fifteen compounds were evaluated in mosquito bioassays with larval mortality rates ranging from ~ 7% to 34% at a concentration of 1 µg/µL and adult mortality ranging from ~10 - 40% at a concentration of 3.125µg.

Technical Abstract: Aedes aegypti is the main mosquito vector for the transmission of serious diseases, including Japanese encephalitis, yellow fever, Zika, and dengue virus. In this paper, a series of novel pyrimidine acyl-hydrazone derivatives were synthesized. Their structures were elucidated by 1H NMR and HRMS. Bioassay results showed that most of the compounds exhibited mosquito larvicidal activity. Compound 4m (N'-(4-bromobenzylidene)-2-((2-(diethylamino)-6-methylpyrimidin-4-yl)oxy)acetohydrazide) exhibited relatively moderate adulticidal activity with 40% mortality at a concentration of 3.125 µg.