Estudo das condições relacionais para síntese do 1,2,3,-triazol 1,4- dissubstituído e avaliação toxicológica.

Abstract

Heterocyclic compounds represent one of the classes that stand out most for having diverse biological activities, so that most drugs have heterocyclic rings in their structure. Among these compounds, 1,2,3-triazoles have been the target of interest for medicinal chemicals as drug candidates for the treatment of various diseases, since they have antifungal, antibacterial, antiviral, anti-inflammatory, antitumor, antiplatelet activity, between others. Furthermore, the 1,2,3-triazole nucleus provides highly efficient and regioselective property results in high yields, making it irreplaceable in various heterocyclic bioactives. Therefore, the objective of this work was to synthesize a new compound 1,2,3-triazole and evaluate its toxicological activity against Artemia salina Leach larvae. N-(azidomethyl)phthalimide was obtained in the form of a white solid with a yield of 87% and, once synthesized, this phthalimide azide was specific and used to study the reaction conditions for the synthesis of the compound 1,2,3- triazole. The results demonstrated that to optimize the reaction conditions, the use of the water: methanol system was foreseen, as well as the basic potassium carbonate species and an ambient temperature of 25°C and after the purification step, the compound 1,2,3-triazole was obtained in 89% yield as a white solid. After optimizing the reaction conditions, the compound 1,2,3- triazole was subjected to a bioassay against Artemia salina larvae, which showed moderate toxicity with an LC50 of 311.94 ppm. This result is important, as there is a demonstration between the toxicity obtained in this bioassay and the biological activity of the compound, therefore, carrying out more in-depth studies on the pharmacological activities of 1,2,3-triazole is essential, as they are considerable related studies show that this pharmacophoric group has great potential to solve several health problems, such as antimicrobial resistance.