Background:
Microbial infections is a global public health problem. The aim of this
work was to synthesize and evaluate the antimicrobial activity of novel triazoles, morpholines and
thiosemicarbazones.
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Methods: Compounds were synthesized using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde
as starting materials. The antimicrobial activity of these compounds against bacteria
and yeast was evaluated by the broth microdilution method.
Results:
The proposed route for synthesis gave high to moderate yields, moreover these compounds
were successfully characterized by 1H NMR, 13C NMR and LC-MS. Antimicrobial testing
indicated that the thiosemicarbazone and morphine derivatives had the best antimicrobial activity
against the microorganisms tested with minimum inhibitory concentrations (MIC) between 0.29
and 5.30 µM. Thiosemicarbazone derivative (12) was able to inhibit the growth of C. tropicalis,
with minimum fungicidal concentration (MFC) of 0.55 µM. In addition, this compound was active
against E. coli, S. aureus and S. epidermidis, with MIC values ranging from 0.29 to 1.11 µM.
Moreover, the morpholine derivative (15) had an MIC value of 0.83 µM against C. albicans and
E. coli.
Conclusion:
We have efficiently synthesized a series of eleven novel triazoles, thiosemicarbazones
and morpholine derivatives using 2,4-Dihydroxyacetophenone and 4-hydroxybenzaldehyde
as starting materials. Thiosemicarbazone derivative (12) showed promising antifungal and antibacterial
activity and these findings suggest that this compound can be used as scaffolds to design
new antimicrobial drugs.
An ethnopharmacological survey indicates that the genus Byrsonima has some medicinal species that are commonly found in the Brazilian Cerrado and has been used as an anti-inflammatory and for gastroduodenal disorders. The aim of this study was to evaluate the anti-inflammatory and antioxidant activity along with qualitative chemical characterization of the methanolic extract of the leaves of Byrsonima verbascifolia (BvME) obtained by exhaustive percolation. The data from the chemical analyses by liquid chromatography-mass spectrometry led to tentative identification of 42 compounds belonging to proanthocyanidins, galloyl quinic acid derivatives, flavonoids, and triterpene glycoside derivatives. BvME contain flavonoids and show an antioxidative activity. The methanolic extract administered intraperitoneally at doses of 50, 100, or 300 mg/kg showed a significant reduction in paw edema and modulated the neutrophil influx in a mouse model. Furthermore, the anti-edematogenic activity of the extract provided in smaller doses (12.5 and 25 mg/kg) was also demonstrated in a mouse paw edema model. The extract inhibited NO production by macrophages induced by lipopolysaccharide. We presume that the anti-inflammatory effects of BvME are due to a combination of compounds present in B. verbascifolia, including catechins (procyanidins), flavonoids, and triterpene glycosides and that these anti-inflammatory actions should be mediated, at least partly, through the inhibition of NO production. This study supports and validates the ethnopharmacological uses of B. verbascifolia as an anti-inflammatory.
Introdução: Os games podem ser vistos como base de engajamento de alunos e professores na escola, criando um ambiente imersivo de aprendizagem. Os conteúdos e tópicos podem ser tratados de forma lúdica, com grandes possibilidades para um melhor desempenho de estudantes no atual contexto cibercultural. Objetivo: Relatar a pesquisa e do desenvolvimento relacionado à utilização de um jogo em realidade virtual, com sistema de captura de movimento Kinect for Windows. Metodologia: Realizou-se atividades de palestras sobre TDIC para professores e cursos sobre jogos educacionais para alunos e professores. Foi desenvolvido um jogo no formato de Quiz com o sistema de captura de movimento Kinect como ferramenta pedagógica em aulas de Química e Biologia. No jogo foram adicionadas 50 questões de Química e 10 de Biologia. O software foi apresentado na escola de Ensino Médio, onde o jogo e seus conteúdos foram avaliados pelos estudantes e professores através de um questionário. Resultados: Segundo a avaliação dos alunos o jogo foi considerando como ótimo para o layout (70%), imagens (80%) e interação (70%) e os professores perceberam um aumento no número de acertos das questões em uma avaliação dos alunos participantes do projeto referentes ao jogo. Conclusão: Os resultados apontam para uma eficácia do jogo considerando uma das possibilidades de utilização das TDIC na educação.
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