Synthesis of New Selenides-1,2,3-Triazoles with Potential Activity against Trypanossoma cruzi

Abstract

Chagas disease, considered by the World Health Organization as a neglected tropical disease, is responsible for the deaths of more than 10,000 people annually. The main drugs used to overcome the disease, Benzonidazole and Nifurtimox, besides being old, have limitations regarding the adverse effects related to the treatment time and consequently their toxicity. Therefore, the need for a new drug to be used against this disease becomes evident. The classes of organoselenium and aromatic heterocycles 1,2,3-triazoles are promising for this issue, profile of both classes for further evaluation against Trypanossoma cruzi, the since both have their known chemistry and antiparasitic activity already described. In this work, the molecular hybridization technique was used in order to combine the individual bioactive protozoan that causes Chagas disease. The methodology used was based on works described in the literature. Initially, benzene azides were synthesized from commercial anilines, while ethynyl(phenyl)selane came from differents aromatic diselenides. With these intermediates, a 1,3-dipolar cycle-addition was performed to obtain the new target molecules 1-phenyl-4-(phenylselanyl)-1H-1,2,3-triazoles with moderate to good yields ranged from 52 to 75%. The characterization of the final molecules is in process and when finished they will be send for evaluation of biological activity. It's possible to conclude that the method used is simple and easy to access, an important factor for potential drugs against neglect diseases. After the assessment of bioactivity, it will be possible to identify the efficiency of these substances, as well as, if necessary, the optimization of their structure.