Resumo

LEAL PINTO, Sandra Milena et al. Antiparasitic activity of novel dihydrodibenzo[c,f]tiazolo[3,2-a] azepin-3(2H)-ones agaisnt Leishmania chagasi and Trypanosoma cruzi. Rev. Univ. Ind. Santander. Salud [online]. 2009, vol.41, n.3, pp.268-274. ISSN 0121-0807.

Introduction: Leishmaniasis and Chagas disease are considered public health problems in several countries and new chemotherapeutic approaches are needed to control these diseases. Objective: The aim of this study was to evaluate the antiparasitic activity of 7 new dihydrodibenzo[c,f]thiazolo[3.2-a]azepin-3(2H)-ones on Leishmania chagasi, Trypanosoma cruzi, and the cytotoxicity on Vero and THP-1 cells. Materials and methods: The antiparasitic activities were determined microscopically counting living parasites compared with untreated control, and the mammalian cell toxicities using the MTT colorimetric test. (Extracellular and intracellular forms of the parasites used and mammalian cells were treated with different concentrations (0.3-600 μM) of compounds for 3-5 days). The activities of the compounds were expressed as the concentration to inhibit 50% percent of parasites (IC₅₀) and the concentration to kill 50% of the mammalian cells (CC₅₀). Results: 4 compounds (4a, 4b, 4d, 4g) were active against T. cruzi epimastigotes with ranges of IC₅₀ from 11.28 to 32.66 μM, and three (4a, 4c, 4g) inhibited the intracellular form (IC₅₀ = 18.42-23.62 μM), with low toxicity on mammalian cells. In L. chagasi, 6 compounds (4a-d, 4g) were active against promastigote forms (IC₅₀= 8.27-28.59 μM). Compound 4d was partially active against intracellular amastigotes of L. chagasi (IC₅₀= 59.36 μM). Conclusions: The compounds 4a and 4g were actives on both T. cruzi and L. chagasi parasites with low toxicity on mammalian cells. Further studies of genotoxicity, mechanisms of action and evaluation of its activity in experimental models are necessaries. Salud UIS 2009; 41: 268-274.

Palavras-chave : Leishmania chagasi; Trypanosoma cruzi; toxicity; dihydrodibenzo[c,f]-thiazolo[3,2-a]azepin-3(2H)- ones; Vero and THP-1 cells.

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