Discovery and structure-activity relationship of Morita-Baylis-Hillman adducts as larvicides against dengue mosquito vector, Aedes aegypti (Diptera: Culicidae)

[Display omitted] Neglected tropical diseases (NTDs) have become a significant public health problem worldwide, notably the life-threatening dengue hemorrhagic fever borne by the Aedes aegypti mosquito. Thus, mosquito vector control measures remain essential in public health vector surveillance and...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2023-07, Vol.90, p.117315-117315, Article 117315
Main Authors: Ricardo dos Santos Correia, Paulo, Duarte de Freitas, Johnnatan, André Zeoly, Lucas, Silva Porto, Ricardo, José da Paz Lima, Dimas
Format: Article
Language:English
Subjects:
Aedes
Aedes aegypti
Animals
Dengue - prevention & control
Insecticides - pharmacology
Larva
Morita-Baylis-Hillman reaction
Mosquito larvicidal assessment
Mosquito Vectors
Neglected tropical diseases
Plant Extracts
Plant Leaves
Scanning electron microscopy analysis
Structure-Activity Relationship
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Summary:[Display omitted] Neglected tropical diseases (NTDs) have become a significant public health problem worldwide, notably the life-threatening dengue hemorrhagic fever borne by the Aedes aegypti mosquito. Thus, mosquito vector control measures remain essential in public health vector surveillance and control to combat Aedes-borne infections. Therefore, a series of MBH adducts were synthesized and assessed towards the fourth instar mosquito larvae, Aedes aegypti, along with the preliminary structure–activity relationship (SAR). Noteworthy, this compound class might be synthetized by an efficient eco-friendly synthesismethod and a rapid route for the synthesis of commercial larvicide through a single synthetic step. The bioassays showed that this compound class is a promising larvicide to control Aedes aegypti mosquito larvae, mainly 3g, with an LC50 of 41.35 µg/mL, which was higher than evaluated positive controls. Nevertheless, it is a viable larvicidalhit candidate for further hit-to-leadproperties optimization of its biphenyl backbone scaffold with enhanced insecticidalbioactivity. Moreover, scanning electron microscopy analysis suggested a disruption of the osmoregulatory/ionoregulatory functions by the complete deterioration of the terminal exoskeleton hindgut and anal papillae. Therefore, this new study shows the larvicidal efficacy of the tested compounds against the Aedes aegypti larvae.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2023.117315