Neglected diseases are caused by infectious and parasitic agents. These diseases are prevalent in tropical and poor areas and in developing countries have been presenting medical relevance. Among the neglected diseases, Chagas disease is endemic in Latin America and has spread to other continents by migratory movements. The research of new antichagasic agents at the national and international levels and in the majority carried out academically, no therapeutic alternatives for the disease have been found yet, thus persisting the urgent need for the discovery and development of new antichagasic agents. The currently strategy in drug discovery involves the choice and selection of specific biochemistry target. In case, sirtuin 2 (silent information regulator 2 – Sir2) were shown to be essential for the in vitro growth of T. cruzi. Sir2 inhibitors like sirtinol showed efficacy against T. cruzi growth. This work presents a comparative of methodologies to synthesize EFsi1 – analogue of sirtinol as a potential antichagasic candidate. The reaction to obtain this product is performed in two stages and in this new proposal it is performed one-pot, using green chemistry principles (scheme 1). For this purpose, a Microwave Synthesis Reactor - Monowave 300 – Anton Paar and ultrasonic cleaner 40 khz Biobase-UC-10A were used. The synthesis on the bench was also performed to establish a comparison. The best result was obtened in microwave with 64% yield in 40 min of the reation than in the bench with 25% yield in 16 horas of the reaction.

New methodology for the synthesis of sirtinol analogues a Sirtuin 2 inhibitor as antichagasic candidates

2019 Fall National Meeting

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