Síntese e avaliação da atividade anti-Trypanosoma cruzi e antifúngica de novos derivados triazólicos

Abstract

In this work ten unprecedented triazolic derivatives with good yields were synthesized. These substances were prepared in six steps using the molecular simplification tool. The products were characterized by infrared spectroscopy, Nuclear Magnetic Resonance Spectroscopy of1H, 13C, DEPT-135, COSY, HSQC and HMBC. Structures of some compounds were confirmed by single crystal X-ray diffraction experiment. Compounds 6-15 were evaluated in vitro against the Y strain of Trypanosoma cruzi protozoan. The results showed that all compounds had inhibition less than 50%, and compound 6 had the best result, with inhibition of 39.5% at 50 M concentration. The antifungal activity of 6-15 was tested for Cryptococcus spp., Candida spp., Microsporum gypseum, Aspergillus fumigatus and Trichophyton rubrum strains. Compound 6 showed higher activity against the dermatophytes Microsporumgypseum (MIC = 32 g / mL) and Trichophyton rubrum (MIC = 32 g/mL). Compound 7 was more active against Trichophyton rubrum (MIC = 64 g/mL), whereas compound 9 was more active against Cryptococcus neoformans (H99) (MIC = 32 g/mL). The results demonstratethat triazole derivatives 6, 7 and 9 are promising prototypes for the development of novel antifungal agents.