bluuebunny/crossref_metadata_2025_split huggingface dataset:
New Fluorous Photoaffinity Labels (F‐PAL) and Their Application in V‐ATPase Inhibition Studies
Authors: Burkard Nadja , Bender Tobias , Westmeier Johannes , Nardmann Christin , Huss Markus , Wieczorek Helmut , Grond Stephanie , von Zezschwitz Paultheo 
Published: March 2010

Abstract(Trifluoromethyl)diazirines are well established photoaffinity labels (PAL) used in biochemical investigations to create covalent ligand‐receptor bonds. Two new diazirinylbenzoic acids 8b,c with perfluorobutyl and perfluorooctyl chains (F‐PAL) were efficiently prepared from p‐bromobenzaldehyde and attached to the highly potent and specific V‐ATPase inhibitors 21‐deoxyconcanolide A (2) and bafilomycin A1 (5), deriving from the natural product pool from Streptomyces producer strains. The labelled derivatives 17 and 18 were efficiently purified by fluorous solid‐phase extraction. Functional biochemical assays with the V‐ATPase holoenzymes proofed strong inhibition activities. So far, radioactive isotopes or biotin‐tags have mainly been used for tracing compounds in photoaffinity studies. The C4F9‐ and C8F17‐fluorous tags aim to enable advantageous separation and identification of labelled peptide fragments by fluorous chromatography followed by MS analysis. Therefore, F‐PAL represents an innovative new concept for binding site determination and should significantly accelerate and simplify such biochemical investigations.
Organocatalyzed Asymmetric Friedel–Crafts Reactions
Authors: Terrasson Vincent , Marcia de Figueiredo Renata , Campagne Jean Marc 
Published: March 2010

AbstractAromatic substitution enables the synthesis of relevant and promising biological entities through the direct synthesis of a range of highly functionalized compounds. Thus, since its discovery and over more than one century, the Friedel–Crafts (F‐C) alkylation has been used for carrying out such a transformation. Despite its aptitude and viability for aromatic substitutions, it is quite surprisingly that catalytic and asymmetric versions of F‐C reactions have only been described in the mid‐1980s. In this microreview, we are planning to underscore the main and recent developments in organocatalyzed F‐C reactions which were published within the 2001–2009 timeframe.
Grecocyclines: New Angucyclines from Streptomyces sp. Acta 1362
Authors: Paululat Thomas , Kulik Andreas , Hausmann Heike , Karagouni Amalia D. , Zinecker Heidi , Imhoff Johannes F. , Fiedler Hans‐Peter 
Published: March 2010

AbstractTwo novel angucyclines were isolated from the streptomycete Acta 1362. The strain was of particular interest regarding the production of characteristic metabolites that were detected by HPLC–diode array profiling of the extracts. Grecocycline A and B were isolated and their structures were determined. Grecocycline A shows cytotoxic activity and grecocycline B inhibits protein tyrosine phosphatase 1B. Moreover, shunt product grecocyline C was isolated and its structure was determined.
Nylon Nanofibrous Biosensors for Glucose Determination
Authors: Scampicchio Matteo , Arecchi Alessandra , Bianco Andrea , Bulbarello Andrea , Bertarelli Chiara , Mannino Saverio 
Published: March 2010

AbstractNanofibrous membranes have been produced by electrospinning to develop first generation glucose biosensors. The direct immobilization of glucose oxidase onto the polyamide nanofibrous surfaces by drop coating revealed a simple and efficient method for the development of sensitive, stable, and reproducible electrochemical biosensors. The biosensor showed a linear response over the range 1–9×10−3 glucose (R2=0.9997) with a sensitivity of 1.11 μA/mM and a limit of detection of 2.5×10−6 M (S/N=3). The uncertainty of repeatability was 2% (RSD%, n=30). After one month of storage, the signal decreased of 35%. The recovery of glucose, evaluated in real samples of honey, was 98% (RSD%=1%, n=3).
Electrocatalytical Oxidation of Nitrite and Its Determination Based on Au@Fe3O4 Nanoparticles
Authors: Yu Chunmei , Guo Jianwei , Gu Haiying 
Published: March 2010

AbstractA promising electrochemical nitrite sensor was fabricated by immobilizing Au@Fe3O4 nanoparticles on the surface of L‐cysteine modified glassy carbon electrode, which was characterized by scanning electron microscopy, X‐ray photoelectron spectroscopy, electrochemical impedance spectroscopy and cyclic voltammetry. The proposed sensor exhibited excellent electrocatalytic activity toward nitrite oxidation. The kinetic parameters of the electrode reaction process were calculated, (1–α)nα was 0.38 and the heterogeneous electron transfer coefficient (k) was 0.13 cm s−1. The detection conditions such as supporting electrolyte and pH value were optimized. Under the optimized conditions, the linear range for the determination of nitrite was 3.6×10−6 to 1.0×10−2 M with a detection limit of 8.2×10−7 M (S/N=3). Moreover, the as‐prepared electrode displayed good stability, repeatability and selectivity for promising practical applications.
Sensitive Determination of Water Insoluble Dyes Used as Marking of Commercial Petroleum Products Using High‐Performance Liquid Chromatography with Electrochemical Detection
Authors: Trindade Magno Aparecido Gonçalves , Zanoni Maria Valnice Boldrin , Matysik Frank‐Michael 
Published: March 2010

AbstractThis paper describes an analytical method using high‐performance liquid chromatographic (HPLC) separation coupled with electrochemical detection to detect three dyes, Solvent Blue 14 (SB‐14), Solvent Blue 35 (SB‐35) and Solvent Red 24 (SR‐24). The dyes were eluted and separated using a reversed‐phase column (C‐8) under isocratic elution with the mobile phase containing a mixture of acetonitrile/ammonium acetate (5.0 mmol L−1) at the ratio of 75 : 25 (v/v). Two sample pretreatment methods were tested and successfully applied to quantify SB14, SB‐35 and SR‐24 dyes in gasoline samples. The proposed method was simple, fast and suitable to detect and quantify marker dyes in gasoline sample at low concentration.
Highly Sensitive and Selective Determination of Dopamine Based on Graphite Nanosheet‐Nafion Composite Film Modified Electrode
Authors: Chen Siming , Yang Wensheng , Chen Xu 
Published: March 2010

AbstractA graphite nanosheet (GNS)‐Nafion modified glassy carbon (GC) electrode was prepared and used for highly sensitive and selective determination of dopamine (DA). The GNS‐Nafion/GC electrode displayed excellent electrocatalytic activities towards DA and ascorbic acid (AA). The selective determination of DA was carried out successfully in the presence of AA by differential pulse voltammetry. High sensitivity (3.695 μA μM−1) and low detection limit (0.02 μM, S/N=3) for the DA detection were obtained. These good properties can be attributed to a large amount of edge plane defects presented on GNSs and the charge‐exclusion and concentration features of Nafion.
An L2‐stable approximation of the Navier–Stokes convection operator for low‐order non‐conforming finite elements
Authors: Ansanay‐Alex G. , Babik F. , Latché J. C. , Vola D. 
Published: March 2010

AbstractWe develop in this paper a discretization for the convection term in variable density unstationary Navier–Stokes equations, which applies to low‐order non‐conforming finite element approximations (the so‐called Crouzeix–Raviart or Rannacher–Turek elements). This discretization is built by a finite volume technique based on a dual mesh. It is shown to enjoy an L2 stability property, which may be seen as a discrete counterpart of the kinetic energy conservation identity. In addition, numerical experiments confirm the robustness and the accuracy of this approximation; in particular, in L2 norm, second‐order space convergence for the velocity and first‐order space convergence for the pressure are observed. Copyright © 2010 John Wiley & Sons, Ltd.
Adaptive finite volume methods with well‐balanced Riemann solvers for modeling floods in rugged terrain: Application to the Malpasset dam‐break flood (France, 1959)
Authors: George D. L. 
Published: March 2010

AbstractThe simulation of advancing flood waves over rugged topography, by solving the shallow‐water equations with well‐balanced high‐resolution finite volume methods and block‐structured dynamic adaptive mesh refinement (AMR), is described and validated in this paper. The efficiency of block‐structured AMR makes large‐scale problems tractable, and allows the use of accurate and stable methods developed for solving general hyperbolic problems on quadrilateral grids. Features indicative of flooding in rugged terrain, such as advancing wet–dry fronts and non‐stationary steady states due to balanced source terms from variable topography, present unique challenges and require modifications such as special Riemann solvers. A well‐balanced Riemann solver for inundation and general (non‐stationary) flow over topography is tested in this context. The difficulties of modeling floods in rugged terrain, and the rationale for and efficacy of using AMR and well‐balanced methods, are presented. The algorithms are validated by simulating the Malpasset dam‐break flood (France, 1959), which has served as a benchmark problem previously. Historical field data, laboratory model data and other numerical simulation results (computed on static fitted meshes) are shown for comparison. The methods are implemented in GEOCLAW, a subset of the open‐source CLAWPACK software. All the software is freely available at www.clawpack.org. Published in 2010 by John Wiley & Sons, Ltd.
How much are clinical fMRI reports influenced by standard postprocessing methods? An investigation of normalization and region of interest effects in the medial temporal lobe
Authors: Beisteiner Roland , Klinger Nicolaus , Höllinger Ilse , Rath Jakob , Gruber Susanne , Steinkellner Thomas , Foki Thomas , Geissler Alexander 
Published: March 2010

AbstractRecent evidence has indicated that standard postprocessing methods such as template‐based region of interest (ROI) definition and normalization of individual brains to a standard template may influence final outcome of functional magnetic resonance imaging investigations. Here, we provide the first comprehensive investigation into whether ROI definition and normalization may also change the clinical interpretation of patient data. A series of medial temporal lobe epilepsy patients were investigated with a clinical memory paradigm and individually delineated as well as template‐based ROIs. Different metrics for activation quantification were applied. Results show that the application of template‐based ROIs can significantly change the clinical interpretation of individual patient data. This relates to sensitivity for brain activation and hemispheric dominance. We conclude that individual ROIs should be defined on nontransformed functional data and that use of more than one metric for activation quantification is beneficial. Hum Brain Mapp, 2010. © 2010 Wiley‐Liss, Inc.
Potential application of population models in the European ecological risk assessment of chemicals II: Review of models and their potential to address environmental protection aims
Authors: Galic Nika , Hommen Udo , Baveco JM (Hans) , van den Brink Paul J 
Published: March 2010

Abstract
Whereas current chemical risk assessment (RA) schemes within the European Union (EU) focus mainly on toxicity and bioaccumulation of chemicals in individual organisms, most protection goals aim at preserving populations of nontarget organisms rather than individuals. Ecological models are tools rarely recommended in official technical documents on RA of chemicals, but are widely used by researchers to assess risks to populations, communities and ecosystems. Their great advantage is the relatively straightforward integration of the sensitivity of species to chemicals, the mode of action and fate in the environment of toxicants, life-history traits of the species of concern, and landscape features. To promote the usage of ecological models in regulatory risk assessment, this study tries to establish whether existing, published ecological modeling studies have addressed or have the potential to address the protection aims and requirements of the chemical directives of the EU. We reviewed 148 publications, and evaluated and analyzed them in a database according to defined criteria. Published models were also classified in terms of 5 areas where their application would be most useful for chemical RA. All potential application areas are well represented in the published literature. Most models were developed to estimate population-level responses on the basis of individual effects, followed by recovery process assessment, both in individuals and at the level of metapopulations. We provide case studies for each of the proposed areas of ecological model application. The lack of clarity about protection goals in legislative documents made it impossible to establish a direct link between modeling studies and protection goals. Because most of the models reviewed here were not developed for regulatory risk assessment, there is great potential and a variety of ecological models in the published literature. Integr Environ Assess Manag 2010;6:338–360. © 2010 SETAC
Reducing environmental impact of dairy cattle: A Czech case study
Authors: Havlikova Martina , Kroeze Carolien 
Published: March 2010

Abstract
We analyze options to reduce the future environmental impact of dairy cattle production, using an optimization model (DAIRY) applied to the Czech Republic. The DAIRY model can be used to calculate the overall environmental impact (OEI). We show that aquatic eutrophication and global warming are the 2 most important problems caused by dairy cattle. These problems are largely caused by nitrate leaching and emissions from animal housing. The DAIRY model indicates that the costs of reducing the OEI in 2020 by 20% are 12 MEuro. It is most cost effective to achieve this reduction by improving the efficiency of animal manure used as fertilizer. We tested the sensitivity of the model to assumptions about the following: 1) the relative importance of environmental problems as expressed in weighting factors, and 2) future cattle numbers and milk yield per milking cow. The first case indicates that disagreement on which problem is most urgent need not lead to disagreement about policies to be undertaken. Regardless of the weighting factors used, aquatic eutrophication and global warming are the most important problems. However, the overall costs of reducing the OEI differ with alternative sets of weighting factors, because the costs of emission reduction differ among pollutants. The second case shows that the DAIRY model results are more sensitive to changes in cattle numbers than to changes in milk yield. This study is the first integrated assessment of dairy cattle production for a Central European country and illustrates how systematic analyses may help to find optimal solutions. Integr Environ Assess Manag 2010;6:367–377. © 2010 SETAC
Contractility modulates cell adhesion strengthening through focal adhesion kinase and assembly of vinculin‐containing focal adhesions
Authors: Dumbauld David W. , Shin Heungsoo , Gallant Nathan D. , Michael Kristin E. , Radhakrishna Harish , García Andrés J. 
Published: March 2010

AbstractActin–myosin contractility modulates focal adhesion assembly, stress fiber formation, and cell migration. We analyzed the contributions of contractility to fibroblast adhesion strengthening using a hydrodynamic adhesion assay and micropatterned substrates to control cell shape and adhesive area. Serum addition resulted in adhesion strengthening to levels 30–40% higher than serum‐free cultures. Inhibition of myosin light chain kinase or Rho‐kinase blocked phosphorylation of myosin light chain to similar extents and eliminated the serum‐induced enhancements in strengthening. Blebbistatin‐induced inhibition of myosin II reduced serum‐induced adhesion strength to similar levels as those obtained by blocking myosin light chain phosphorylation. Reductions in adhesion strengthening by inhibitors of contractility correlated with loss of vinculin and talin from focal adhesions without changes in integrin binding. In vinculin‐null cells, inhibition of contractility did not alter adhesive force, whereas controls displayed a 20% reduction in adhesion strength, indicating that the effects of contractility on adhesive force are vinculin‐dependent. Furthermore, in cells expressing FAK, inhibitors of contractility reduced serum‐induced adhesion strengthening as well as eliminated focal adhesion assembly. In contrast, in the absence of FAK, these inhibitors did not alter adhesion strength or focal adhesion assembly. These results indicate that contractility modulates adhesion strengthening via FAK‐dependent, vinculin‐containing focal adhesion assembly. J. Cell. Physiol. 223:746–756, 2010. © 2010 Wiley‐Liss, Inc.
Curcumin stimulates glucose uptake through AMPK‐p38 MAPK pathways in L6 myotube cells
Authors: Kim Ji Hae , Park Ji Man , Kim Eung‐Kyun , Lee Jung Ok , Lee Soo Kyung , Jung Jin Hee , You Ga Young , Park Sun Hwa , Suh Pann‐Ghill , Kim Hyeon Soo 
Published: March 2010

AbstractCurcumin has been shown to exert a variety of beneficial human health effects. However, mechanisms by which curcumin acts are poorly understood. In this study, we report that curcumin activated AMP‐activated protein kinase (AMPK) and increased glucose uptake in rat L6 myotubes. In addition, curcumin activated the mitogen‐activated protein kinase kinase (MEK)3/6‐p38 mitogen‐activated protein kinase (MAPK) signaling pathways in the downstream of the AMPK cascade. Moreover, inhibition of either AMPK or p38 MAPK resulted in blockage of curcumin‐induced glucose uptake. Furthermore, the administration of curcumin to mice increased AMPK phosphorylation in the skeletal muscles. Taken together, these results indicate that the beneficial health effect of curcumin can be explained by its ability to activate AMPK‐p38 MAPK pathways in skeletal muscles. J. Cell. Physiol. 223:771–778, 2010. © 2010 Wiley‐Liss, Inc.
Diclofenac removal from water by ozone and photolytic TiO2 catalysed processes
Authors: García‐Araya Juan F. , Beltrán Fernando J. , Aguinaco Almudena 
Published: March 2010

AbstractBACKGROUND: The aim of this work was to establish the efficiency of single ozonation at different pH levels (5, 7 and 9) and with different TiO2 photolytic oxidizing systems (O2/UV‐A/TiO2, O3/UV‐A/TiO2 or UV‐A/TiO2) for diclofenac removal from water, with especial emphasis on mineralization of the organic matter.RESULTS: In the case of single ozonation processes, results show fast and practically complete elimination of diclofenac, with little differences in removal rates that depend on pH and buffering conditions. In contrast, total organic carbon (TOC) removal rates are slow and mineralization degree reaches 50% at best. As far as photocatalytic processes are concerned, diclofenac is completely removed from the aqueous solutions at high rates. However, unlike single ozonation processes, TOC removal can reach 80%.CONCLUSION: In single ozonation processes, direct ozone reaction is mainly responsible for diclofenac elimination. Once diclofenac has disappeared, its by‐products are removed by reaction with hydroxyl radicals formed in the ozone decomposition and also from the reaction of diclofenac with ozone. In the photocatalytic processes hydroxyl radicals are responsible oxidant species of diclofenac removal as well as by‐products. Copyright © 2010 Society of Chemical Industry
[4+2] Cycloaddition of α,β‐unsaturated acid anhydrides to 2‐furylpiperidin‐4‐ones: The short route to annulated 8,10a‐epoxypyrido[2,1‐a]isoindoles
Authors: Zubkov Fedor I. , Airiyan Inga K. , Dzyubenko Anastasiya A. , Yudina Nataliya I. , Zaytsev Vladimir P. , Nikitina Eugeniya V. , Varlamov Alexey V. , Khrustalev Victor N. , Grudinin Dmitry G. 
Published: March 2010

Abstract
magnified image A one‐step preparation procedure of 8,10a‐epoxypyrido[2,1‐a]isoindoles and their 7‐carboxylic derivatives is reported. The key synthetic step includes the intramolecular exo‐Diels–Alder reaction (IMDAF) of N‐furfurylacrylamide, produced in situ from 2‐furylpiperidin‐4‐ones and α,β‐unsaturated acid anhydrides. The synthesis of the title compounds can be performed under mild conditions with a high level of regio‐ and stereoselectivity. The same strategy has been successfully used for the synthesis of 9,11a‐epoxyimidazo[4′,5′:3,4]pyrido[2,1‐a]isoindole‐8‐carboxylic acid from maleic anhydride and the spinacine derivatives – 4‐(2‐furyl)‐4,5,6,7‐tetrahydro‐3H‐imidazo[4,5‐c]pyridines. J. Heterocyclic Chem., (2010).
Synthesis of new 1,2,3‐triazolo[1,5‐a]quinazolinones
Authors: Pokhodylo Nazariy T. , Matiychuk Vasyl S. 
Published: March 2010

Abstract
magnified image Synthesis of novel 3‐substituted‐1,2,3‐triazolo[1,5‐a]quinazolinones in high yields was performed via anionic hetero‐domino reaction of appropriate substituted 2‐azidobenzoates prepared from isatines and acetonitriles activated by 1,3‐thiazole, 1,3‐benzothiazole, 1,3,4‐oxadiazole, and 1,2,4‐oxadiazole rings. It was shown that acetonitriles exhibited high reactivity and were convenient methylenic compounds for such reactions providing rapid structural variation. J. Heterocyclic Chem., (2010).
A green procedure for the synthesis of 1,8‐dioxodecahydroacridine derivatives under microwave irradiation in aqueous media without catalyst
Authors: Tang Zi‐Qiang , Chen Yan , Liu Chang‐Ning , Cai Ke‐Ying , Tu Shu‐Jiang 
Published: March 2010

Abstract
magnified image A green procedure for the synthesis of 1,8‐dioxo‐decahydroacridine derivatives is developed under microwave irradiation without catalyst in water. This method provides several advantages such as excellent yields (86–96%), simple workup procedure, and environment friendliness. J. Heterocyclic Chem., (2010).
Tandem Michael addition/imino‐nitrile cyclization synthesis of 2‐amino‐6‐(1‐aryl‐5‐methyl‐1H‐1,2,3‐triazol‐4yl)‐4‐phenylpyridine‐3‐carbonitrile
Authors: Dong Heng‐Shan , Wang Hui‐Cheng , Gao Zhong‐Lian , Li Rong‐Shan , Cui Fu‐Hong 
Published: March 2010

Abstract
magnified image Several 2–amino‐6‐(1‐aryl‐5‐methyl‐1H‐1,2,3‐triazol‐4‐yl)‐4‐phenylpyridine‐3‐carbonitrile have been synthesized by Tandem Michael addition/imino‐nitrile cyclization and the structures of these compounds were established by MS, IR, CHN, and 1H NMR spectral data. The crystal structure of 2‐amino‐6‐[1‐(4‐methoxyphenyl)‐5‐methyl‐1H‐1,2,3‐triazol‐4‐yl]‐4‐phenylpyridine‐3‐carbonitrile was established by X‐ray diffraction. J. Heterocyclic Chem., (2010).
Synthesis and antibacterial screening of new 4‐((5‐(difluoromethoxy)‐1H‐benzo[d]imidazol‐2‐ylthio)methyl)tetrazolo[1,5‐a]quinoline derivatives
Authors: Sonar Swapnil S. , Sadaphal Sandip A. , Pokalwar Rajkumar U. , Shingate Bapurao B. , Shingare Murlidhar S. 
Published: March 2010

Abstract
magnified image A method for the synthesis of previously unknown heterocyclic systems 4‐((5‐(difluoromethoxy)‐1H‐benzo[d]imidazol‐2‐ylthio)methyl)tetrazolo[1,5‐a]quinolines derivatives 6 has been developed based on various substitutes 2‐chloroquinoline‐3‐carbaldehydes 1 via the consecutive steps of conversion into tetrazolo[1,5‐a]quinoline‐4‐carbaldehyde 2 on treatment with sodium azide which upon reduction to the corresponding alcohol derivatives 3, conversion to chlorides 4 with thionyl chloride followed by the coupling with 5‐(difluoromethoxy)‐1H‐benzo[d]imidazole‐2‐thiol 5. The synthesized titled compounds (6a, 6b, 6c, 6d, 6e) were screened for the antibacterial activity against gram positive and gram negative bacteria. J. Heterocyclic Chem., (2010).