Avaliação de atividade anti-leishmania de novos análogos nitroimidazóis sulfonamídicos

Abstract

Neglected diseases are diseases that mainly affect underdeveloped tropical countries, due to high economic inequality and difficult access to health services, diagnosis and treatment. The drugs used to treat these diseases are restricted and research for the development of new treatments unfortunately does not arouse the interest of pharmaceutical industries due to the low purchasing power of the population. Among the main neglected diseases that occur in Brazil, we can mention leishmaniasis, which are prevalent and constitute a serious public health problem. Therefore, studies for new drug candidates for these types of diseases are of paramount importance. In this work, 25 sulfonamide hybrid analogues 2-nitroimidazoles were analyzed, previously synthesized by means of bioisosteric substitution of the triazole group with the amide group of Benznidazole, and using the sulfonamide group present in oryzalin, in the ring connected in this group that has the structural modifications, which aims to evaluate the antileishmania activity in amastigote forms of L. amazonensis of these compounds. Of which the compound stands out 6 and 25 that showed better CI50 compared to the reference compound, pentamidine. In addition to compounds 5, 9, 15, 24 and 26, which showed similar activity to the reference compound pentamidine. These analogues can be analyzed in future in vivo tests to be able to trace possible mechanisms of action.