Abstract
AbstractAedes 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 has created a need to develop new mosquitocidal agents for effective control operations. A series of benzothiazole-piperidine derivatives (1-24) were investigated for their larvicidal and adulticidal effects on Ae. aegypti It was observed that compounds 2, 4, 6, 7, 8, 11 and 13 showed notable larvicidal activity. Furthermore, compounds 6 and 10 showed promising adulticidal activity. Based on the mosquitocidal 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 active compounds showed reasonable interactions with critical 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 2, 4, 6, 7, 8, 10, 11 and 13 stand out as candidates for further studies.
Highlights
Mosquitoes are one of the most dangerous insect vectors and infectious disease carriers in developing countries [1]
Chemical insecticides are considered as the first option for reducing vector-borne disease but evolving resistance caused by cytochrome P450 monooxygenases (P450s), which are capable of metabolizing many insecticides, as well as decreases in target site sensitivity can limit the success of insecticide treatment [8,9,10]
Compounds carrying benzothiazole and piperidine rings were investigated for first instar larvicidal activity and adulticidal activity against Ae. aegypti
Summary
Mosquitoes are one of the most dangerous insect vectors and infectious disease carriers in developing countries [1]. Aedes aegypti L. transmits yellow fever, dengue fever, chikungunya, and more recently, Zika virus [2]. Fifty seven compounds were identified in silico as possible inhibitors of the cholesterol-binding capacity of SCP-2 from the library of 16000 compounds [20]. Targeting this cholesterol transport pathway associated with AeSCP2 could be an alternative target for the development of specific mosquitocidal agents. Molecular docking studies were performed for the most effective compounds within the active site of AeSCP2 (PDB code: 1PZ4) to provide a mechanistic approach for further studies [30]
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