Search results for "45"
showing 10 items of 1896 documents
CCDC 1553488: Experimental Crystal Structure Determination
2018
Related Article: Djamille Azazna, Marine Lafosse, Julie Rivollier, Jialan Wang, Imen Ben Cheikh, Michel Meyer, Pierre Thury, Jean-Pierre Dognon, Gaspard Huber, Marie-Pierre Heck|2018|Chem.-Eur.J.|24|10793|doi:10.1002/chem.201801468
Charged Tags for the Identification of Oxidative Drug Metabolites Based on Electrochemistry and Mass Spectrometry
2020
Abstract Most of the active pharmaceutical ingredients like Metoprolol are oxidatively metabolized by liver enzymes, such as Cytochrome P450 monooxygenases into oxygenates and therefore hydrophilic products. It is of utmost importance to identify the metabolites and to gain knowledge on their toxic impacts. By using electrochemistry, it is possible to mimic enzymatic transformations and to identify metabolic hot spots. By introducing charged‐tags into the intermediate, it is possible to detect and isolate metabolic products. The identification and synthesis of initially oxidized metabolites are important to understand possible toxic activities. The gained knowledge about the metabolism will…
Phenotypic and genotypic study on antibiotic resistance and pathogenic factors of Staphylococcus aureus isolates from small ruminant mastitis milk in…
2021
Staphyloccoccus aureus is the major cause of mastitis in small ruminants in the Mediterranean farms causing severe losses to dairy industry. Antibiotic treatment has been the most common approach to control these infections. Aim of this study was to investigate antimicrobial resistance (AMR), virulence factors and biofilm-related genes of 84 Sicilian strains of S. aureus isolated from sheep and goats milk during two different periods δT1 (2006-2009) and δT2 (2013-2015). Kirby Bauer method and Polymerase Chain Reaction (PCR) were utilized to monitor AMR and related genes (mecA, tetK, tetM, ermA, ermC). Moreover, toxin genes (tsst-1, sea-see, seg-sej, and sep) and biofilm genes (bap, ica, sas…
Statistics of nonlinear stochastic dynamical systems under Lévy noises by a convolution quadrature approach
2010
This paper describes a novel numerical approach to find the statistics of the non-stationary response of scalar non-linear systems excited by L\'evy white noises. The proposed numerical procedure relies on the introduction of an integral transform of Wiener-Hopf type into the equation governing the characteristic function. Once this equation is rewritten as partial integro-differential equation, it is then solved by applying the method of convolution quadrature originally proposed by Lubich, here extended to deal with this particular integral transform. The proposed approach is relevant for two reasons: 1) Statistics of systems with several different drift terms can be handled in an efficie…
Quantum graphs with mixed dynamics: the transport/diffusion case
2013
We introduce a class of partial differential equations on metric graphs associated with mixed evolution: on some edges we consider diffusion processes, on other ones transport phenomena. This yields a system of equations with possibly nonlocal couplings at the boundary. We provide sufficient conditions for these to be governed by a contractive semigroup on a Hilbert space naturally associated with the system. We show that our setting is also adequate to discuss specific systems of diffusion equations with boundary delays.
Synthesis and in vitro antileukemic activity of new 4-triazenopyrazole derivatives
2003
Several new 4-(3,3-dimethyltriazeno)-5-benzamidopyrazole derivatives were prepared by reacting 4-diazo-5-benzamidopyrazole derivatives with dimethylamine. The compounds were tested at 10 microM for their vitro antileukemic activity against K562 (Human chronic myelogenous leukemia) and Raji (human Burkitt limphoma ) cell lines. Dacarbazine and methotrexate were used for comparative purpose. The 3-methyl-4-(3,3-dimethyltriazeno)-5-(substituted benzamido)pyrazoles, bearing the pyrazole nucleus free at 1 position, resulted more active than the 1-(substituted phenyl)-3-methyl-4-(3,3-dimethyltriazeno)-5-benzamidopyrazoles. Dacarbazine at 10 microM showed no activity in the above tests. The observ…
Stereoselective metabolism of dibenz(a,h)anthracene to trans-dihydrodiols and their activation to bacterial mutagens.
1990
Dibenz(a,h)anthracene (DBA), a carcinogenic, polycyclic aromatic hydrocarbon ubiquitous in the environment, is metabolized by the hepatic microsomal fraction of immature Sprague-Dawley rats pretreated with Aroclor 1254 to 27 ethyl acetate-extractable metabolites. More than half of these metabolites (51%) consisted of trans-1,2-; -3,4-; and -5,6-dihydrodiols including their identified secondary metabolites. The three trans-dihydrodiols (4.9, 15.8, and 0.6% of total metabolic conversion) were highly enriched in their R,R enantiomers (85, 71, and 98%) as determined by high performance liquid chromatography on suitable chiral stationary phases. This is explained on the basis of the stereoselect…
Metabolic activation of dibenzo[a,l]pyrene by human cytochrome P450 1A1 and P450 1B1 expressed in V79 Chinese hamster cells.
1999
Metabolic activation of the strongly carcinogenic polycyclic aromatic hydrocarbon (PAH) dibenzo[a,l]pyrene (DB[a,l]P) and its trans-8,9-dihydrodiol (trans-8,9-diol) catalyzed by human cytochromes P450 (P450) 1A1 and 1B1 was investigated. DNA binding of DB[a,l]P in mammalian cell lines has previously been shown to be preferentially mediated by fjord region DB[a,l]P-11,12-dihydrodiol 13,14-epoxides (DB[a,l]PDE). In order to elucidate different capabilities of both P450 enzymes for metabolic activation of DB[a, l]P V79 Chinese hamster cells, stably expressing human P450s 1A1 or 1B1 have been exposed to the parent PAH or its racemic trans-8, 9-diol. For this purpose, synthesis and spectroscopic…
Steviol glycosides and bioactive compounds of a beverage with exotic fruits and Stevia rebaudiana Bert. as affected by thermal treatment
2020
The aim of this study was to investigate the effects of thermal processing on physicochemical properties, steviol glycosides, bioactive compounds, and antioxidant capacity degradation of a beverage based on exotic fruit juices, orange juice, açaí, and oat and sweetened with Stevia rebaudiana water extracts at different concentrations. The experimental design comprised a response surface methodology according to a central composite face-centered design. The variable ranges were 60–99°C, 0.25–15 min, 0–2.5% Stevia percentage. This design was used to determine the optimal thermal processing-Stevia concentration in order to obtain the best retention of bioactive compounds and physicochemical pr…
Combined Anchoring: Prosecution and defense claims as sequential anchors in the courtroom
2021
Purpose When making judgements under uncertainty not only lay people but also professional judges often rely on heuristics like a numerical anchor (e.g., a numerical sentencing demand) to generate a numerical response. As the prosecution has the privilege to present its demand first, some scholars have speculated about an anchoring���based unfair disadvantage for the defence (who has the last albeit less effective word in court). Despite the plausibility of this reasoning, it is based on a hitherto untested assumption that the first of two sequential anchors exerts a greater influence on a later judgement (a primacy effect). We argue that it is also conceivable that the last word in court h…