DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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Resultados da Pesquisa
Item Synthesis and microbiological activity of some 2H-1,4-benzothiazin-3-one derivatives.(2000) Guarda, Vera Lúcia de Miranda; Perrissin, Monique; Thomasson, François; Ximenes, Eulália Camelo Pessoa de Azevedo; Galdino, Suely Lins; Pitta, Ivan da Rocha; Luu-Duc, CuongThe synthesis and physicochemical properties of 4-butyl-2H-benzo[1,4]thiazin-3-one derivatives are described. These new compounds were synthesised by alkylation in 4-N position and acylation and/or alkylation of 6-NH2 by phase transfer catalysis. Acid hydrolysis of 6-alkylacylamino group yielded 6-alkylamino-4-butyl-2H-benzo[1,4]thiazin-3-ones. The antimicrobial in vitro activity was determined on five compounds.Item Chemical constituents from branches of Maytenus gonoclada (Celastraceae) and evaluation of antimicrobial activity.(2011) Silva, Fernando César; Duarte, Lucienir Pains; Silva, Grácia Divina de Fátima; Vieira Filho, Sidney Augusto; Lula, Ivana Silva; Takahashi, Jacqueline Aparecida; Sallum, William S. T.Seis triterpenos pentacíclicos isolados dos galhos de Maytenus gonoclada (Celastraceae), incluindo todos os dados de RMN do novo composto 3-oxo-12α,29-diidroxifriedelano são aqui relatados. A estereoquímica do novo friedelano foi estabelecida por dados de RMN bidimensional (HSQC, HMBC e NOESY), e sua massa molecular confirmada por espectrometria de massas (ESI). Testes de atividade antimicrobiana usando método de difusão em disco e de macrodiluição foram realizados contra as bactérias Escherichia coli, Citrobacter freundii e Bacillus cereus, e contra o fungo Candida albicans. O triterpeno 3-oxo-12a-hidroxifriedelano mostrou resultado positivo contra C. albicans.Item In vitro activity of 2-pyridinecarboxylic acid against trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus.(2011) Corrêa, Paulo Roberto Ceridóreo; Pinto, Artur da Silveira; Silva, Grácia Divina de Fátima; Vieira Filho, Sidney Augusto; Duarte, Lucienir Pains; Ogatta, Sueli Fumie YamadaThe effect of 2-pyridinecarboxylic acid (picolinic acid) on trypanosomes of the subgenus Schizotrypanum isolated from the bat Phyllostomus hastatus was determined in this study. Picolinic acid, at 50 g mL-1, inhibited epimastigote growth by 99% after 12 days incubation. In addition, trypomastigote motility decreased by 50% after 6h and completely after 24h in the presence of 50 g mL-1 picolinic acid. The 50% cytotoxic concentration on HEp-2 cell line was 275 g mL-1 after 4 days incubation. Altogether, these results indicate higher toxicity against trypanosomes. The inhibitory effect of picolinic acid on epimastigote growth can be partially reversed by nicotinic acid and L tryptophan, suggesting a competitive inhibition. Furthermore, two anti-Trypanosoma (Schizotrypanum) cruzi drugs were also evaluated with regard to bat trypanosome growth. Benznidazole, at 50 g mL-1, inhibited epimastigote growth by 90% after 12 days incubation. Nifurtimox, at the same concentration, caused 96% growth inhibition after four days incubation. Corroborating a previous study, bat trypanosomes are a good model for screening new trypanocidal compounds. Moreover, they can be used to study many biological processes common to human pathogenic trypanosomatids.