934 resultados para 2,3-dimetoxy-8-oxoberberine
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A new 2,3,4,6-tetra-O-(3-nitropropanoyl)-O-β-D-glucopyranoside anomer was isolated from the roots of Heteropteris aphrodisiaca and characterized by spectroscopic methods. Activity against Staphylococcus aureus, Bacillus subtilis, Candida albicans, C. parapsilosis, C. krusei, and C. tropicalis was demonstrated.
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This study evaluated the fluoride intake from dentifrices with different fluoride concentrations ([F]) by children aged 24-36 months, as well as the influence of the dentifrice flavor in the amount of fluoride ingested during toothbrushing. Thirty-three children were randomly divided into 3 groups, according to the [F] in the dentifrices: G-A (523 μgF/g), G-B (1,062 μgF/g) and G-C (1,373 μgF/g). Dentifrices A and B are marketed for children, while dentifrice C is a regular product. The amount of F ingested was indirectly obtained, subtracting the amount expelled and the amount left on the toothbrush from the amount initially loaded onto the brush. The results were analyzed by ANOVA, Tukey's test and linear regression analysis (p < 0.05). Children ingested around 60% of the dentifrice loaded onto the brush, but no significant differences were seen among the groups (p > 0.05). Mean daily fluoride intake from dentifrice for G-A, G-B and G-C was 0.022 a, 0.032 a and 0.061 b mg F/kg body weight, respectively (p < 0.01). There was a strong positive correlation (r = 0.86, p < 0.0001) between the amount of dentifrice used and the amount of fluoride ingested during toothbrushing. The results indicate the need for instructing children's parents and care givers to use a small amount of dentifrice (< 0.3 g) to avoid excessive ingestion of fluoride. The use of low-[F] dentifrices by children younger than 6 years also seems to be a good alternative to minimize fluoride intake. Dentifrice flavor did not influence the percentage of fluoride intake.
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The dielectric properties of the 0.65[Pb(Mg 1/3Nb 2/3)O 3]-0.35PbTiO 3 ferroelectric ceramic composition were investigated viewing the capability to be used for tunable microwave applications. The dielectric response has been studied for three selected temperatures (300 K, 370 K and 400 K), below the paraelectric- ferroelectric phase transition temperature, as a function of the applied 'bias' electric field. The obtained dielectric tunability was found to be around 60 %, under an electric field of 19 kV/cm, which makes the studied ceramic composition an excellent candidate for application in the electro-electronic industry, as tunable devices. © 2010 IEEE.
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In this article, we investigate the geometry of quasi homogeneous corank one finitely determined map germs from (ℂn+1, 0) to (ℂn, 0) with n = 2, 3. We give a complete description, in terms of the weights and degrees, of the invariants that are associated to all stable singularities which appear in the discriminant of such map germs. The first class of invariants which we study are the isolated singularities, called 0-stable singularities because they are the 0-dimensional singularities. First, we give a formula to compute the number of An points which appear in any stable deformation of a quasi homogeneous co-rank one map germ from (ℂn+1, 0) to (ℂn, 0) with n = 2, 3. To get such a formula, we apply the Hilbert's syzygy theorem to determine the graded free resolution given by the syzygy modules of the associated iterated Jacobian ideal. Then we show how to obtain the other 0-stable singularities, these isolated singularities are formed by multiple points and here we use the relation among them and the Fitting ideals of the discriminant. For n = 2, there exists only the germ of double points set and for n = 3 there are the triple points, named points A1,1,1 and the normal crossing between a germ of a cuspidal edge and a germ of a plane, named A2,1. For n = 3, there appear also the one-dimensional singularities, which are of two types: germs of cuspidal edges or germs of double points curves. For these singularities, we show how to compute the polar multiplicities and also the local Euler obstruction at the origin in terms of the weights and degrees. © 2013 Pushpa Publishing House.
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Incluye Bibliografía
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Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
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Coordenação de Pessoal de Nível Superior (CAPES)
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This work describes the synthesis of a series of sialylmimetic neoglycoconjugates represented by 1,4-disubstituted 1,2,3-triazole-sialic acid derivatives containing galactose modified at either C-1 or C-6 positions, glucose or gulose at C-3 position, and by the amino acid derivative 1,2,3-triazole fused threonine-3-O-galactose as potential TcTS inhibitors and anti-trypanosomal agents. This series was obtained by Cu(I)-catalysed azide-alkyne cycloaddition reaction ('click chemistry') between the azido-functionalized sugars 1-N(3)-Gal (commercial), 6-N(3)-Gal, 3-N(3)-Glc and 3-N(3)-Gul with the corresponding alkyne-based 2-propynyl-sialic acid, as well as by click chemistry reaction between the amino acid N(3)-ThrOBn with 3-O-propynyl-GalOMe. The 1,2,3-triazole linked sialic acid-6-O-galactose and the sialic acid-galactopyranoside showed high Trypanosoma cruzi trans-sialidase (TcTS) inhibitory activity at 1.0 mM (approx. 90%), whilst only the former displayed relevant trypanocidal activity (IC(50) 260 mu M). These results highlight the 1,2,3-triazole linked sialic acid-6-O-galactose as a prototype for further design of new neoglycoconjugates against Chagas' disease. (C) 2011 Elsevier Ltd. All rights reserved.
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Five 2-hydroxy-3-substituted-aminomethyl naphthoquinones, nine 1,2,3-triazolic para-naphthoquinones, five nor-beta-lapachone-based 1,2,3-triazoles, and several other naphthoquinonoid compounds were synthesized and evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease, continuing our screening program for new trypanocidal compounds. Among all the substances, 16-18, 23, 25-29 and 30-33 were herein described for the first time and fifteen substances were identified as more potent than the standard drug benznidazole, with IC50/24 h values in the range of 10.9-101.5 mu M. Compounds 14 and 19 with Selectivity Index of 18.9 and 6.1 are important structures for further studies. (C) 2012 Elsevier Masson SAS. All rights reserved.
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Glasses in the system [Na2S](2/3)[(B2S3)(x)(P2S5)(1-x)](1/3) (0.0 <= x <= 1.0) were prepared by the melt quenching technique, and their properties were characterized by thermal analysis and impedance spectroscopy. Their atomic-level structures were comprehensively characterized by Raman spectroscopy and B-11, P-31, and Na-23 high resolution solid state magic-angle spinning (MAS) NMR techniques. P-31 MAS NMR peak assignments were made by the presence or absence of homonuclear indirect P-31-P-31 spin-spin interactions as detected using homonuclear J-resolved and refocused INADEQUATE techniques. The extent of B-S-P connectivity in the glassy network was quantified by P-31{B-11} and B-11{P-31} rotational echo double resonance spectroscopy. The results clearly illustrate that the network modifier alkali sulfide, Na2S, is not proportionally shared between the two network former components, B and P. Rather, the thiophosphate (P) component tends to attract a larger concentration of network modifier species than predicted by the bulk composition, and this results in the conversion of P2S74-, pyrothiophosphate, Na/P = 2:1, units into PS43-, orthothiophosphate, Na/P = 3:1, groups. Charge balance is maintained by increasing the net degree of polymerization of the thioborate (B) units through the formation of covalent bridging sulfur (BS) units, B S B. Detailed inspection of the B-11 MAS NMR spectra reveals that multiple thioborate units are formed, ranging from neutral BS3/2 groups all the way to the fully depolymerized orthothioborate (BS33-) species. On the basis of these results, a comprehensive and quantitative structural model is developed for these glasses, on the basis of which the compositional trends in the glass transition temperatures (T-g) and ionic conductivities can be rationalized. Up to x = 0.4, the dominant process can be described in a simplified way by the net reaction equation P-1 + B-1 reversible arrow P-0 + B-4, where the superscripts denote the number of BS atoms for the respective network former species. Above x = 0.4, all of the thiophosphate units are of the P-0 type and both pyro-(B-1) and orthothioborate (B-0) species make increasing contributions to the network structure with increasing x. In sharp contrast to the situation in sodium borophosphate glasses, four-coordinated thioborate species are generally less abundant and heteroatomic B-S-P linkages appear to not exist. On the basis of this structural information, compositional trends in the ionic conductivities are discussed in relation to the nature of the charge-compensating anionic species and the spatial distribution of the charge carriers.
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The magnetic moments of the low-lying spin-parity J(P) = 1/2(-), 3/2(-) Lambda resonances, like, for example, Lambda(1405) 1/2(-), Lambda(1520) 3/2(-), as well as their transition magnetic moments, are calculated using the chiral quark model. The results found are compared with those obtained from the nonrelativistic quark model and those of unitary chiral theories, where some of these states are generated through the dynamics of two hadron coupled channels and their unitarization.
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MeOH extract from the leaves of Plectranthus barbatus Andrews (Lamiaceae), showed in vitro anti-trypanosomal activity. The bioassay-guided fractionation resulted in the isolation of a gallic acid derivative, identified as 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG), after thorough NMR and MS spectral analysis. Finally, this compound was tested against trypomastigote forms of T. cruzi and displayed an EC50 value of 67 mu M, at least 6.6-fold more effective than the standard drug benznidazole. This is the first occurrence of PGG in the Plectranthus genus and the first anti-parasitic activity described for PGG in the literature.
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A very fast, easy and efficient synthesis is described for a novel and biologically important class of 1,4-disubstituted-4-(5-pyrrolidin-2-one)-1,2,3-triazoles by an ultrasound-assisted one-pot, three-step click reaction sequence of 5-[(trimethylsilyl)ethynyl]pyrrolidin-2-one with organic azides mediated by catalytic Cu-I salts.