20 resultados para antiprotozoal
Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates
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The present work reports on the synthesis, biological assaying and docking studies of a series of 12 aryl thiosemicarbazones, which were planned to act over two main enzymes, cruzain and trypanothione reductase. These enzymes are used as targets of trypanocidal activity in Chagas disease control with a minimal mutagenic profile. Three p-nitroaromatic thiosemicarbazones showed high activity against Trypanosoma cruzi in in vitro assays (IC50 < 57 μM), and no mutagenic profile was observed in micronucleous tests. Although the in vitro inhibition test showed that 10-μM doses of eight compounds inhibited cruzain activity, no correlation was found between cruzain inhibition and trypanocidal activity. © 2013 Elsevier Masson SAS. All rights reserved.
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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Violacein is a deeply violet pigment produced by Chromobacterium violaceum, an ubique tropical and subtropical bacterium. This molecule presents many biological activities including antimicrobial, antimycotic, antiviral, antiprotozoal and antitumoral. Important reports pointed to a considerable bactericide activity, which brings an extremely necessary quest. This work evaluated the resistance of some bacterias of interest veterinary. It was obtained significant inhibition activity against Staphylococcus aureus came from bovine mastitis. It was also obtained important synergic relations when violacein and penicillin or cloranphenicol are combined
