Avaliação da atividade antileishmania in vitro de compostos imidazo[2,1-b]tiazóis sintéticos

Abstract

Leishmaniases are neglected tropical diseases for which the current treatments are highly toxic, require long-term administration and are costly. They are also subject to parasitic resistance. The cutaneous form is the most prevalent, particularly in South American countries such as Brazil. Therefore, developing safer and more effective therapies is essential. In this regard, synthetic heterocyclic compounds containing selenium and sulphur atoms exhibit promising antileishmania activity. The aim of this project was to investigate the in vitro antileishmania activity of synthetic compounds containing selenium and sulfur with imidazo[2,1-b]thiazole structures. The compounds were tested against promastigotes and intracellular amastigotes of Leishmania amazonensis, and their cytotoxicity was evaluated in a mouse fibroblast cell line. The compounds exhibited activity against the promastigote forms of L. amazonensis with minimal reduction in NIH/3T3 fibroblast viability, and some demonstrated activity against the intracellular amastigote forms. Compound S61 exhibited the greatest activity against intracellular amastigote forms, demonstrating an IC₅₀ of 5.66 μM and a selectivity index of 17.9. Most of the compounds exhibited desirable physicochemical properties that are compatible with the development of new drugs. The results of this project made it possible to screen promising compounds that will be evaluated in future in vitro and in vivo studies for their potential molecular targets, with the aim of developing new therapeutic alternatives for leishmaniasis.