O-alquilação de um composto fenólico e ensaios de toxicidade frente a larvas de Artemia salina Leach e teste de antividade antifúgica contra cepas do gênero Candida spp.

Abstract

The pharmaceutical industry has an arsenal of drugs used in the treatment of various diseases. However, some of these drugs only relieve symptoms, have high costs and side effects. One alternative is the use of natural products. And a class of natural products that has been drawing the attention of several research groups, due to its abundance in nature and varied pharmacological actions, are the phenolic compounds. Therefore, it is necessary to evaluate the toxicity and activity of these phenolic compounds through toxicological bioassay with Artemia salina larvae, aiming an application against pathogenic fungal species. This concern is due to the growth of the cases of infections caused in the world associated with the high resistance of some fungi against the action of some antifungal drugs. Therefore, the objective of the present work was to study the reaction conditions of the alkylation reaction of a phenolic compound, besides carrying out toxicological bioassays of these compounds against A. salina larvae and and to evaluate its antifungal activity. The O-alkylation reaction was used, in which compounds 1a and 1b were used as alkylating agents leading to the formation of 2 derivatives of the phenolic compound, which were purified and characterized by spectroscopic techniques. Then, the toxicological bioassay was performed against A. salina larvae aiming to find the LC50. The antifungal activity assays were done by the microdilution technique in wells, which aimed to determine the MIC against fungi of the genus Candida spp. At the end of the reactions the compounds were obtained in good yields, ranging from 85 to 95% and the spectroscopic data corroborate the obtaining of these compounds. The LC50 were less than 100 g/mL, showing high toxicity. The antifungal activity tests revealed that the compounds present antifungal activity against some strains of the Candida spp. genus, especially compound 3a. Thus, it is notorious the importance of further studies that aim to continue the discovery of the activities that these molecules and their derivatives may express, in order to search for new drug candidates.