Herein, we report the design, synthesis and trypanocidal activity of some novel trisubstituted imidazole derivatives. These heterocyclic derivatives were structurally planned by exploring the concept of molecular hybridisation between two arylhydrazones derived from megazol, which has potent trypanocidal activity. The trypanocidal activity of these triarylimidazole derivatives was evaluated aga...

With the aim of finding new chemical entities based on coumarin and chalcone scaffolds, new hybrid compounds 2-5 were designed and synthesized. The trypanocidal activity of these compounds was tested against the epimastigote, trypomastigote and amastigote stages of the Trypanosoma cruzi parasite. Cytotoxicity assays were also performed in RAW 264.7 and VERO cells. Compound 5 presented the highe...

some medicinal plants are a potential source of new drugs, in order to improve the treatment of chagas disease whose treatment is still a challenge. in this study, the in vitro anti-epimastigote activity of certain fractions of achillea biebersteinii, a. millefolium, satureja mutica and s. macrantha was evaluated. diethyl ether fractions of achillea species and acetone fractions of satureja spe...

Higher plants are a potential source of new drugs to improve the treatment of Chagase disease, which is affecting 16-18 million people, with more than 100 million exposed to the risk of infection (Ambrozin et al., 2004; Coura & Castro, 2002). Current therapy is unsatisfactory, because the only two drugs available, benznidazole and nifortimox possess severe side effects and their activity is lim...

We have synthesized a series of dimers of (+)-(7R,11R)-huprine Y and evaluated their activity against Trypanosoma brucei, Plasmodium falciparum, rat myoblast L6 cells and human acetylcholinesterase (hAChE), and their brain permeability. Most dimers have more potent and selective trypanocidal activity than huprine Y and are brain permeable, but they are devoid of antimalarial activity and remain...

We report the trypanocidal activity of quinonemethide triterpenoids isolated from root extracts of Cheiloclinium cognatum, a plant of the Hippocrateaceae family, collected in the Cerrado Reserve at Universidade Federal de Goiás, Brazil. The trypanocidal activity assays showed an effect on the blood trypomastigote forms of the Y strain of Trypanosoma cruzi where tingenone and tingenol demonstrat...

A group of bis-cationic imidazo[1,2-a]pyridinium salts and related compounds, some of which exhibit in vivo trypanocidal activity, have been investigated for induction of petite mutagenesis in Saccharomyces cerevisiae. All of the compounds which are active trypanocides induce mutagenesis. There appears to be a correlation between trypanocidal activity and mutagenic activity which may have its s...

Some medicinal plants are a potential source of new drugs, in order to improve the treatment of Chagas disease whose treatment is still a challenge. In this study, the in vitro anti-epimastigote activity of certain fractions of Achillea biebersteinii, A. millefolium, Satureja mutica and S. macrantha was evaluated. Diethyl ether fractions of Achillea species and acetone fractions of Satureja spe...

Normal, resident and inflammatory mouse peritoneal macrophages can be induced to display microbicidal activity against trypomastigotes of Trypanosoma cruzi by exposure to products from antigen-pulsed, sensitized spleen cell populations. Optimal macrophage microbicidal activity was achieved by constant exposure and daily renewal of the spleen cell factors. Macrophages obtained after an intraperi...