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ARS Home » Southeast Area » Gainesville, Florida » Center for Medical, Agricultural and Veterinary Entomology » Mosquito and Fly Research » Research » Publications at this Location » Publication #351924
Title: Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

Author
item SEVER, BELGIN - Anadolu Universtiy
item ALTINTOP, MEHLIKA DILEK - Anadolu Universtiy
item OZDEMIR, AHMET - Anadolu Universtiy
item Tabanca, Nurhayat
item ESTEP, ALDEN - Navy Entomology Center Of Excellence, Cmave Detachment
item Becnel, James
item BLOOMQUIST, JEFFREY - University Of Florida

Submitted to: Open Chemistry
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 12/26/2018
Publication Date: 6/25/2019
Citation: Sever, B., Altintop, M., Ozdemir, A., Tabanca, N., Estep, A.S., Becnel, J.J., Bloomquist, J.R. 2019. Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents. Open Chemistry. 17(1):288-294. https://doi.org/10.1515/chem-2019-0027.
DOI: https://doi.org/10.1515/chem-2019-0027

Interpretive Summary: Mosquito-borne diseases are a global problem and a continued threat to public health. Emergence of resistance to the majority of existing compounds has prompted a continued demand for new insecticides. In this study, a series of benzothiazole-piperidine derivatives were investigated for their activity against the major vector mosquito Aedes aegypti. Several active compounds were effective in increasing mosquito adulticidal and larvicidal activity and may lead to the development of new effective public health pesticides.

Technical Abstract: Aedes aegypti is associated with the transmission of numerous human and animal diseases, such as yellow fever, dengue fever, chikungunya, and more recently Zika virus. Emerging insecticide resistance during the fight with the mosquitoes has created an instant need to develop new mosquitocidal agents. A series of benzothiazole-piperidine derivatives (1-24) were investigated for their larvicidal and adulticidal effects on Ae. aegypti. It was observed that compounds 11, 6, 4, 2, 13, 8 and 7 showed notable larvicidal activity. Furthermore, compounds 6 and 10 showed promising adulticidal activity. Based on antimosquito properties of these compounds, docking studies were also carried out in the active site of the AeSCP2 enzyme to explore any insights into further in vitro enzyme studies. Docking results indicated that all these compounds showed reasonable interactions with proper residues in the active site of this enzyme. This outcome suggested that these compounds might show their larvicidal and adulticidal effects via the inhibition of AeSCP2. According to in vitro and in silico studies, compounds 10, 11, 6, 4, 2, 13, 8, and 7 stand out as candidates for further studies.