973 resultados para SUBSTITUTED 1,3-DIENES
Resumo:
Esta pesquisa busca reconstruir um período da história de Israel os seis anos de governo da Rainha Atalia, em Judá (841-836 aC) tendo como base a análise exegética e histórica de 2Rs11,1-3.13-16. O cenário e o estilo de 2Rs 11 permitem afirmar que o autor pertencia ao círculo dos escribas da corte ou da instituição religiosa. A pesquisa recorre às ocorrências dos termos rainha-mãe e gebirah, presentes no Antigo Testamento, e às contribuições das tradições dos países vizinhos, a fim de explicar a ascensão de Atalia ao trono de Judá. Atalia ocupou a função de rainha-mãe. Com isso competia-lhe a importante função de cuidar da estabilidade da realeza e, eventualmente, exercer a regência até que a ocupação por direito se tornasse viável. Atalia foi soberana por seis anos em Judá. Para manter-se tanto tempo no poder, Atalia contou com forças aliadas, ou seja, um grupo que a garantiu no trono. Atalia é filha da casa de Omri com mãe israelita de fé javista. A vinda de Atalia para Jerusalém é resultado de um período de paz entre os dois reinos irmãos. A durabilidade de seu governo deve-se, não a atos de beligerância, e provavelmente sim à sua exemplar administração, baseada principalmente na atividade comercial, favorecida pela posição estratégica de Jerusalém no cruzamento de importantes rotas comerciais da época. Atalia estava preparada para liderar um país com metas no comércio internacional.
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A prominent feature of several type of cancer is cachexia. This syndrome causes a marked loss of lean body mass and muscle wasting, and appears to be mediated by cytokines and tumour products. There are several proteases and proteolytic pathways that could be responsible for the protein breakdown. In the present study, we investigated whether caspases are involved in the proteolytic process of skeletal muscle catabolism observed in a murine model of cancer cachexia (MAC16), in comparison with a related tumour (MAC13), which does not induce cachexia. Using specific peptide substrates, there was an increase of 54% in the proteolytic activity of caspase-1, 84% of caspase-8, 98% of caspase-3 151% to caspase-6 and 177% of caspase-9, in the gastrocnemius muscle of animals bearing the MAC16 tumour (up to 25% weight loss), in relation to muscle from animals bearing the MAC13 tumour (1-5% weight loss). The dual pattern of 89 kDa and 25 kDa fragmentation of poly (ADP-ribose) polymerase (PARP) occurred in the muscle samples from animals bearing the MAC16 tumour and with a high amount of caspase-like activity. Cytochrome c was present in the cytosolic fractions of gastrocnemius muscles from both groups of animals, suggesting that cytochrome c release from mitochondria may be involved in caspase activation. There was no evidence for DNA fragmentation into a nucleosomal ladder typical of apoptosis in the muscles of either group of mice. This data supports a role for caspases in the catabolic events in muscle involved in the cancer cachexia syndrome. © 2001 Cancer Research Campaign.
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A rapid one-pot synthesis of 3-alkyl-5-[(Z)-arylmethylidene]-1,3-thiazolidine-2,4-dionesis described that occurs in recyclable ionic liquid [bmim]PF6 (1-butyl-3-methylimidazolium hexafluorophosphate).Significant rate enhancement and good selectivity have been observed.
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Human adrenomedullin (AM) is a 52-amino acid peptide belonging to the calcitonin peptide family, which also includes calcitonin gene-related peptide (CGRP) and AM2. The two AM receptors, AM(1) and AM(2), are calcitonin receptor-like receptor (CL)/receptor activity-modifying protein (RAMP) (RAMP2 and RAMP3, respectively) heterodimers. CGRP receptors comprise CL/RAMP1. The only human AM receptor antagonist (AM(22-52)) is a truncated form of AM; it has low affinity and is only weakly selective for AM(1) over AM(2) receptors. To develop novel AM receptor antagonists, we explored the importance of different regions of AM in interactions with AM(1), AM(2), and CGRP receptors. AM(22-52) was the framework for generating further AM fragments (AM(26-52) and AM(30-52)), novel AM/alphaCGRP chimeras (C1-C5 and C9), and AM/AM(2) chimeras (C6-C8). cAMP assays were used to screen the antagonists at all receptors to determine their affinity and selectivity. Circular dichroism spectroscopy was used to investigate the secondary structures of AM and its related peptides. The data indicate that the structures of AM, AM2, and alphaCGRP differ from one another. Our chimeric approach enabled the identification of two nonselective high-affinity antagonists of AM(1), AM(2), and CGRP receptors (C2 and C6), one high-affinity antagonist of AM(2) receptors (C7), and a weak antagonist selective for the CGRP receptor (C5). By use of receptor mutagenesis, we also determined that the C-terminal nine amino acids of AM seem to be responsible for its interaction with Glu74 of RAMP3. We provide new information on the structure-activity relationship of AM, alphaCGRP, and AM2 and how AM interacts with CGRP and AM(2) receptors.
Resumo:
Controlled polymerization of 2-chloro-1,3-butadiene using reversible addition–fragmentation chain transfer (RAFT) polymerization has been demonstrated for the first time. 2-Chloro-1,3-butadiene, more commonly known as chloroprene, has significant industrial relevance as a crosslinked rubber, with uses ranging from adhesives to integral automotive components. However, problems surrounding the inherent toxicity of the lifecycle of the thiourea-vulcanized rubber have led to the need for control over the synthesis of poly(2-chloro-1,3-butadiene). To this end, four chain transfer agents in two different solvents have been trialed and the kinetics are discussed. 2-Cyano-2-propylbenzodithioate (CPD) is shown to polymerize 2-chloro-1,3-butadiene in THF, using AIBN as an initiator, with complete control over the target molecular weight, producing polymers with low polydispersities (Mw/Mn < 1.25 in all cases).
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Partially supported by the Technical University of Gabrovo under Grant C-801/2008
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Oxazepam (4a) has been used as overall starting material in the synthesis of novel 2-substituted 1,4-benzodiazepines. By reacting Oxazepam 4a with commercially available hydrazines, hydrazides, semicarbazide, aminoguanidine and N,N-dimethylamino aniline in ethanol under acetic conditions, a series of diazenyl-1,4-benzodiazepines 5a-5i and 2-amino- 1,4-benzodiazepine 5k were obtained in good yields. These novel compounds served as new chemical entities (NCE) for testing in mice. The diazo-benzodiazepine 5d has shown a promising antidepressant effect in initial experiments in vivo at a dose of 5 mg/kg. The highly coloured 2-aminobenzodiazepine derivative 5k showed over a dose range from 5-50 mg/kg an analgesic effect in mice. © Singh et al.
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The work on CERP monitoring item 3.1.3.5 (Marl prairie/slough gradients) is being conducted by Florida International University (Dr Michael Ross, Project Leader), with Everglades National Park (Dr. Craig Smith) providing administrative support and technical consultation. As of January 2006 the funds transferred by ACOE to ENP, and subsequently to FIU, have been entirely expended or encumbered in salaries or wages. The project work for 2005 started rather late in the fiscal year, but ultimately accomplished the Year 1 goals of securing a permit to conduct the research in Everglades National Park, finalizing a detailed scope of work, and sampling marsh sites which are most easily accessed during the wet season. 46 plots were sampled in detail, and a preliminary vegetation classification distinguished three groups among these sites (Sawgrass marsh, sawgrass and other, and slough) which may be arranged roughly along a hydrologic gradient from least to most persistently inundated . We also made coarser observations of vegetation type at 5-m intervals along 2 transects totaling ~ 5 km. When these data were compared with similar observations made in 1998-99, it appeared that vegetation in the western portion of Northeast Shark Slough (immediately east of the L-67 extension) had shifted toward a more hydric type during the last 6 years, while vegetation further east was unchanged in this respect. Because this classification and trend analysis is based on a small fraction of the data set that will be available after the first cycle of sampling (3 years from now), the results should not be interpreted too expansively. However, they do demonstrate the potential for gaining a more comprehensive view of marsh vegetation structure and dynamics in the Everglades, and will provide a sound basis for adaptive management.
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Trägerband: Inc. qu. 960; Vorbesitzer: Zacharias Konrad von Uffenbach
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We investigated controls on the water chemistry of a South Ecuadorian cloud forest catchment which is partly pristine, and partly converted to extensive pasture. From April 2007 to May 2008 water samples were taken weekly to biweekly at nine different subcatchments, and were screened for differences in electric conductivity, pH, anion, as well as element composition. A principal component analysis was conducted to reduce dimensionality of the data set and define major factors explaining variation in the data. Three main factors were isolated by a subset of 10 elements (Ca2+, Ce, Gd, K+, Mg2+, Na+, Nd, Rb, Sr, Y), explaining around 90% of the data variation. Land-use was the major factor controlling and changing water chemistry of the subcatchments. A second factor was associated with the concentration of rare earth elements in water, presumably highlighting other anthropogenic influences such as gravel excavation or road construction. Around 12% of the variation was explained by the third component, which was defined by the occurrence of Rb and K and represents the influence of vegetation dynamics on element accumulation and wash-out. Comparison of base- and fast flow concentrations led to the assumption that a significant portion of soil water from around 30 cm depth contributes to storm flow, as revealed by increased rare earth element concentrations in fast flow samples. Our findings demonstrate the utility of multi-tracer principal component analysis to study tropical headwater streams, and emphasize the need for effective land management in cloud forest catchments.