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	Provedor de dados BJPS (2) Autor Jin,Qing-Hao (2) Liu,Bing-Yu (2) Xia,Ya-Nan (2) Chen,Wen-Bo (1) Fu,Zhi-Yang (1) Guan,Li-Ping (1) Jiang,Hai-Ying (1) Mais... Palavra-chave Antibacterial activity (1) CDC25B (1) Dioxoindolin-N-phenylacetamide (1) Enzyme kinetics (1) Flavonoids (1) Isoprenyloxyflavones (1) PTP1B (1) Phosphatase inhibitors (1) Synthesis (1) Mais... Tipo do documento Info:eu-repo/semantics/article (2) Ano 2020 (2) País Brazil (2) Idioma Inglês (2)		Ordenar por:  Relevância Autor Título Ano Registros recuperados: 2 Primeira ... 1 ... Última Synthesis and antibacterial activity of a series novel 5,7-diisoprenyloxyflavone derivatives BJPS Jin,Qing-Hao; Fu,Zhi-Yang; Xia,Ya-Nan; Liu,Bing-Yu; Jiang,Hai-Ying. In the present study, a series of novel 5,7-diisoprenyloxyflavone derivatives were designed, synthesized, and evaluated for their antibacterial activity. Most of these compounds displayed significant antibacterial effects against Gram-positive bacteria, especially against strains of multidrug-resistant clinical isolates. Compounds 4c, 4g, 4i, 4j, 4k, 4l, 4n, 4q and 4t showed high levels of antimicrobial activity against Staphylococcus aureus RN4220 with minimum inhibitory concentrations of 4.0-20 µM. Compound 4k showed the most potent activity among these compounds against all multidrug-resistant clinical isolates tested. Unfortunately, none of the compounds were active against Gram-negative bacteria at the doses of 24-164 µM. Tipo: Info:eu-repo/semantics/article Palavras-chave: Flavonoids; Synthesis; Isoprenyloxyflavones; Antibacterial activity. Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100541 Biological evaluation of 2,3-dioxoindolin-N-phenylacetamide derivatives as potent CDC25B and PTP1B phosphatase inhibitors BJPS Jin,Qing-Hao; Chen,Wen-Bo; Xia,Ya-Nan; Liu,Bing-Yu; Guan,Li-Ping. A series of 2,3-dioxoindolin-N-phenylacetamide derivatives was evaluated for inhibitory activity against CDC25B and PTP1B enzymes. Most of the derivatives showed inhibitory activity against CDC25B (IC50 = 3.2-23.2 µg/mL) and PTP1B (IC50 = 2.9-21.4 µg/mL). Compound 2h showed the most inhibitory activity in vitro with IC50 values of 3.2 and 2.9 µg/mL against CDC25B and PTP1B, respectively, compared with the reference drugs Na3VO4 (IC50 = 2.7 µg/mL) and oleanolic acid (IC50 = 2.3 µg/mL). The results of selectivity experiments showed that the 2,3-dioxoindolin-N-phenylacetamide derivatives were selective inhibitors against CDC25B and PTP1B. Enzyme kinetic experiments demonstrated that compound 2h was a specific inhibitor with the typical characteristics of a... Tipo: Info:eu-repo/semantics/article Palavras-chave: Dioxoindolin-N-phenylacetamide; CDC25B; PTP1B; Phosphatase inhibitors; Enzyme kinetics. Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100500 Registros recuperados: 2 Primeira ... 1 ... Última

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