AGUIAR, C. E. R.; http://lattes.cnpq.br/7023888006326924; AGUIAR, Carlos Eduardo Rodrigues.
Resumo:
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.