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

Abstract

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.