Probaren hizkuntzak ebaluazioen emaitzetan duen eragina : irakaskuntza elebiduneko ikasleek nazioarteko probetan duten errendimenduari buruzko ikerketa

Existe una versi??n en espa??ol, con el t??tulo "Influencia de la lengua de la prueba en los resultados de las evaluaciones : investigaci??n sobre el rendimiento con pruebas internacionales del alumnado en programas de educaci??n biling??e"

Antioxidant and antimicrobial properties of 2-(4,5-dihydro-1H-pyrazol-1-yl)-pyrimidine and 1-carboxamidino-1H-pyrazole derivatives

Five previously synthesized 4-trifluoromethyl-2-(5-aryl-3-styryl-1H-pyrazol-1yl)-pyrimidines and six 5-aryl-3-styryl-1-carboxamidino-1H-pyrazole derivatives were screened for their antioxidant proprieties. The antioxidant activities were evaluated by using the DPPH and the HRP/luminol/H2O2 chemiluminescence assay systems and for their antimicrobial activity (MIC). The results were good for those series in some concentration in comparison with the standards.

4-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)benzoic acid: X-ray and DFT-calculated structure

In the title compound, C(11)H(7)NO(4), there is a dihedral angle of 45.80 (7)degrees between the planes of the benzene and maleimide rings. The presence of O-H...O hydrogen bonding and weak C-H...O interactions allows the formation of R (3) 3(19) edge-connected rings parallel to the (010) plane. Structural, spectroscopic and theoretical studies were carried out. Density functional theory (DFT) optimized structures at the B3LYP/6-311 G(d,p) and 6-31++G(d,p) levels are compared with the experimentally determined molecular structure in the solid state. Additional IR and UV theoretical studies allowed the presence of functional groups and the transition bands of the system to be identified.

2-(4-Methylphenyl)-1H-anthraceno-[1,2-d]imidazole-6,11-dione: a fluorescent chemosensor

In the title compound, C(22)H(14)N(2)O(2), the five rings of the molecule are not coplanar. There is a significant twist between the four fused rings, which have a slightly arched conformation, and the pendant aromatic ring, as seen in the dihedral angle of 13.16 (8)degrees between the anthraquinonic ring system and the pendant aromatic ring plane.

Regiospecific synthesis of 5-trichloromethyl-1H-pyrazole and 1H-pyrazole-5-carboxylic ester derivatives

Reaction of 1,1,1-trichloro-4-methoxy-3-penten-2-one (1) with hydrazines (2a-h) (NH2NHR, R = H, Me, t-Bu, Ph, 4-NO2-C6H4, C6F5, CO2Me, CONH2) under differing conditions regiospecifically affords different pyrazole derivatives, 3-methyl-5-trichloromethyl-5-hydroxy-4,5-dihydropyrazoles (3a, d-h), 3-methyl-5-trichloromethyl-1H-pyrazoles (4a,b,d-g) and 5-carboxyethyl-3-methyl-1H-pyrazoles (5a-e). The structural assignments were based on the analysis of their H-1/C-13 NMR and ESI-MS data.

Antioxidant Capacity of 2-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenylthiazoles

The antioxidant capacity of 2-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenylthiazoles was evaluated. The values of antioxidant capacities of compounds 2d and 2e were found to be, respectively, 2,700 +/- 150 and 3,135 +/- 230 TE by the ORAC method, corresponding to a significant antioxidant capacity.

Efficient sonochemical synthesis of novel 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides

An Ultrasound-assisted preparation of a series of novel 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides that proceeds via the efficient reaction of chalcones with aminoguanidine hydrochloride under clean conditions is described. (C) 2009 Elsevier B.V. All rights reserved.

Environmentally friendly sonocatalysis promoted preparation of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles

An efficient and green synthesis of thiocarbamoyl-3,5-diaryl-4,5-dihydro-1 H-pyrazoles via the condensation of chalcones with thiosemicarbazide in ethanol and KOH under ultrasound irradiation is reported. The products were isolated in good yields after short reaction times. (C) 2009 Elsevier B.V. All rights reserved.

Synthesis, antichagasic in vitro evaluation, cytotoxicity assays, molecular modeling and SAR/QSAR studies of a 2-phenyl-3-(1-phenyl-1H-pyrazol-4-yl)-acrylic acid benzylidene-carbohydrazide series

Chagas disease (American trypanosomiasis) is one of the most important parasitic diseases with serious social and economic impacts mainly on Latin America. This work reports the synthesis, in vitro trypanocidal evaluation, cytotoxicity assays, and molecular modeling and SAR/QSAR studies of a new series of N-phenylpyrazole benzylidene-carbohydrazides. The results pointed 6k (X = H, Y = p-NO(2), pIC(50) = 4.55 M) and 6l (X = F, Y = p-CN, pIC(50) = 4.27 M) as the most potent derivatives compared to crystal violet (pIC(50) = 3.77 M). The halogen-benzylidene-carbohydrazide presented the lowest potency whereas 6l showed the most promising pro. le with low toxicity (0% of cell death). The best equation from the 4D-QSAR analysis (Model 1) was able to explain 85% of the activity variability. The QSAR graphical representation revealed that bulky X-substituents decreased the potency whereas hydrophobic and hydrogen bond acceptor Y-substituents increased it. (C) 2008 Elsevier Ltd. All rights reserved.

Espetroscopia (1H) por ressonância magnética do disco intervertebral lombar no adulto e sua aplicação na rotina imagiológica

Objetivos – Demonstrar o potencial da espetroscopia (1H) por ressonância magnética na doença degenerativa discal lombar e defender a integração desta técnica na rotina clínico‑imagiológica para a precisa classificação da involução vs degenerescência dos discos L4‑L5 e L5‑S1 em doentes com lombalgia não relacionável com causa mecânica. Material e métodos – O estudo incluiu 102 discos intervertebrais lombares de 123 doentes. Foram estudados 61 discos de L4‑L5, 41 discos de L5‑S1 e 34 discos de D12‑L1. Utilizou‑se um sistema de ressonância magnética de 1,5 T e técnica monovoxel. Obtiveram‑se os rácios [Lac/Nacetyl] e [Nacetyl/(Lac+Lípidos)] e aplicou‑se a ressonância de lípidos para avaliar a bioquímica do disco com o fim de conhecer o estado de involução vs degenerescência que o suscetibilizam para a instabilidade e sobrecarga. Avaliou‑se o comportamento dos rácios e do teor lipídico dos discos L4‑L5‑S1 e as diferenças apresentadas em relação a D12‑L1. Foi também realizada a comparação entre os discos L4‑L5, L5‑S1 e D12‑L1 na ponderação T2 (T2W), segundo a classificação ajustada (1‑4) de Pfirrmann. Resultados – Verificou‑se que os rácios e o valor dos lípidos dos discos L4‑L5‑S1 apresentaram diferenças estatisticamente significativas quando relacionados com os discos D12‑L1. O rácio [Lac/Nacetyl] em L4‑L5‑S1 mostrou‑se aumentado em relação a D12‑L1 (p=0,033 para os discos com grau de involução [1+2] e p=0,004 para os discos com grau [3+4]). Estes resultados sugerem que a involução vs degenerescência dos discos nos graus mais elevados condiciona um decréscimo do pico do Lactato. O rácio [Nacetyl/(Lac+Lip)] discrimina os graus de involução [1+2] do [3+4] no nível L4‑L5, apresentando os valores dos rácios (média 0,65 e 0,5 respetivamente com p=0,04). O rácio médio de [Nacetyl/(Lac+Lip)] dos discos L4‑L5 foi 1,8 vezes mais elevado do que em D12‑L1. O espetro lipídico em L4‑L5‑S1 nos graus mais elevados não mostrou ter uma prevalência constante quanto às frequências de ressonância. Conclusão – A espetroscopia (1H) dos discos intervertebrais poderá ter aplicação na discriminação dos graus de involução vs degenerescência e representar um contributo semiológico importante em suplemento à ponderação T2 convencional. As ressonâncias de lípidos dos discos L4‑L5 e L5‑S1, involuídos ou degenerados, devem ser avaliadas em relação a D12‑L1, utilizando este valor como referência, pois este último é o nível considerado estável e com baixa probabilidade de degenerescência.

Antifungal action of three (Z)-5-amino-N'-aryl-1-methyl-1H-imidazole-4-carbohydrazonamides

[Excerpt] The incidence of fungal infections has greatly increased in patients under sustained immunosuppression with considerable risk associated. Difficulties regarding prompt diagnosis and the limited therapeutic options dictate high mortality rates. Available antifungals display substantial toxicity, a predictable consequence of the cellular structure of the organisms involved, reduced spectrum of activity, and drug interactions. Our group had previously identified three (Z)-5-amino-N'-aryl-1-methyl-1H-imidazole-4-carbohydrazonamides 1 [aryl= phenyl (1a), 4-fluorophenyl (1b), 3fluorophenyl (1c)] as potent antifungal agents.1 (...)

1H Magnetresonanzspektroskopie der gesunden Leber und von malignen Leberläsionen bei 3.0 Tesla

Magdeburg, Univ., Med. Fak., Diss., 2015

Neurochemical profile of the developing mouse cortex determined by in vivo 1H NMR spectroscopy at 14.1 T and the effect of recurrent anaesthesia.

The neurochemical profile of the cortex develops in a region and time specific manner, which can be distorted by psychiatric and other neurological pathologies. Pre-clinical studies often involve experimental mouse models. In this study, we determined the neurochemical profile of C57BL/6 mice in a longitudinal study design to provide a reference frame for the normal developing mouse cortex. Using in vivo proton NMR spectroscopy at 14 T, we measured the concentrations of 18 metabolites in the anterior and posterior cortex on postnatal days (P) 10, 20, 30, 60 and 90. Cortical development was marked by alterations of highly concentrated metabolites, such as N-acetylaspartate, glutamate, taurine and creatine. Regional specificity was represented by early variations in the concentration of glutamine, aspartate and choline. In adult animals, regional concentration differences were found for N-acetylaspartate, creatine and myo-inositol. In this study, animals were exposed to recurrent isoflurane anaesthesia. Additional experiments showed that the latter was devoid of major effects on behaviour or cortical neurochemical profile. In conclusion, the high sensitivity and reproducibility of the measurements achieved at 14 T allowed us to identify developmental variations of cortical areas within the mouse cortex.

In vivo quantification of neuro-glial metabolism and glial glutamate concentration using 1H-[13C] MRS at 14.1T.

Astrocytes have recently become a major center of interest in neurochemistry with the discoveries on their major role in brain energy metabolism. An interesting way to probe this glial contribution is given by in vivo (13) C NMR spectroscopy coupled with the infusion labeled glial-specific substrate, such as acetate. In this study, we infused alpha-chloralose anesthetized rats with [2-(13) C]acetate and followed the dynamics of the fractional enrichment (FE) in the positions C4 and C3 of glutamate and glutamine with high sensitivity, using (1) H-[(13) C] magnetic resonance spectroscopy (MRS) at 14.1T. Applying a two-compartment mathematical model to the measured time courses yielded a glial tricarboxylic acid (TCA) cycle rate (Vg ) of 0.27 ± 0.02 μmol/g/min and a glutamatergic neurotransmission rate (VNT ) of 0.15 ± 0.01 μmol/g/min. Glial oxidative ATP metabolism thus accounts for 38% of total oxidative metabolism measured by NMR. Pyruvate carboxylase (VPC ) was 0.09 ± 0.01 μmol/g/min, corresponding to 37% of the glial glutamine synthesis rate. The glial and neuronal transmitochondrial fluxes (Vx (g) and Vx (n) ) were of the same order of magnitude as the respective TCA cycle fluxes. In addition, we estimated a glial glutamate pool size of 0.6 ± 0.1 μmol/g. The effect of spectral data quality on the fluxes estimates was analyzed by Monte Carlo simulations. In this (13) C-acetate labeling study, we propose a refined two-compartment analysis of brain energy metabolism based on (13) C turnover curves of acetate, glutamate and glutamine measured with state of the art in vivo dynamic MRS at high magnetic field in rats, enabling a deeper understanding of the specific role of glial cells in brain oxidative metabolism. In addition, the robustness of the metabolic fluxes determination relative to MRS data quality was carefully studied.

Detection of neuronal activity and metabolism in a model of dehydration-induced anorexia in rats at 14.1 T using manganese-enhanced MRI and 1H MRS.

In this study, hypothalamic activation was performed by dehydration-induced anorexia (DIA) and overnight food suppression (OFS) in female rats. The assessment of the hypothalamic response to these challenges by manganese-enhanced MRI showed increased neuronal activity in the paraventricular nuclei (PVN) and lateral hypothalamus (LH), both known to be areas involved in the regulation of food intake. The effects of DIA and OFS were compared by generating T-score maps. Increased neuronal activation was detected in the PVN and LH of DIA rats relative to OFS rats. In addition, the neurochemical profile of the PVN and LH were measured by (1) H MRS at 14.1T. Significant increases in metabolite levels were measured in DIA and OFS relative to control rats. Statistically significant increases in γ-aminobutyric acid were found in DIA (p=0.0007) and OFS (p<0.001) relative to control rats. Lactate increased significantly in DIA (p=0.03), but not in OFS, rats. This work shows that manganese-enhanced MRI coupled to (1) H MRS at high field is a promising noninvasive method for the investigation of the neural pathways and mechanisms involved in the control of food intake, in the autonomic and endocrine control of energy metabolism and in the regulation of body weight.