Larvicidal activity of thiazolidinedione derivatives against Aedes aegypti larvae and toxicological studies with zebrafish embryos


BACKGROUND: Diseases caused by arboviruses are currently a worldwide public health problem. These diseases have the Aedes aegypti mosquito as the main transmission vector, and the main strategy to combat their spread is the interruption of the mosquito life cycle in its early stages. In this study, we synthesized thirteen thiazolidinedione derivatives (3a-3m) that were applied in a larvicide-based strategy against the Ae. aegypti vector and submitted to evaluation of toxicological effects. RESULTS: Microwave process intensification was utilized for the synthesis of thiazolidinedione derivatives (3a-3m). One thiazolidinedione derivative stands out (3a) with lethal concentrations (LC50-24 h) of 7.71 μg mL-1 (32.16 μmol L-1). It showed embryotoxicity to zebrafish at concentrations up to 1.0 μg mL-1 and mortality from 3.1 up to 100 μg mL-1. No biochemical disturbances occurred based on GST and LDH measurements. A para-substituted chlorine atom instead of hydrogen improves toxicity profile. CONCLUSION: The substitution pattern with a chlorine atom suggests a larvicidal activity. From the compounds tested, (Z)-5-(4-chlorobenzylidene)thiazolidine-2,4-dione (3a) was the most effective against Ae. Aegypti, showing embryotoxicity to zebrafish.

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.docx to .pdf supporting information and a little correction on the manuscript


Supplementary material

Supporting Information
Data containing NMR spectra.