bluuebunny/crossref_metadata_2025_split huggingface dataset:
Effects of ketoconazole or rifampin on the pharmacokinetics of tivozanib hydrochloride, a vascular endothelial growth factor receptor tyrosine kinase inhibitor
Authors: Cotreau Monette M. , Siebers Nicholas M. , Miller James , Strahs Andrew L. , Slichenmyer William 
Published: July 2014

AbstractThe vascular endothelial growth factor (VEGF) pathway is associated with the promotion of endothelial cell proliferation, migration, and survival necessary for angiogenesis. VEGF and its three receptor isoforms are often overexpressed in many human solid tumors. Tivozanib is a potent, selective inhibitor of VEGF receptors 1, 2, and 3, with a long half‐life. The purpose of these studies was to evaluate the effect of ketoconazole, a potent inhibitor of CYP3A4, and rifampin, a potent inducer of CYP3A4, on the pharmacokinetics of tivozanib. Two phase I, open‐label, 2‐period, single‐sequence studies evaluated the effect of steady‐state ketoconazole (NCT01363778) or rifampin (NCT01363804) on the pharmacokinetic profile, safety, and tolerability of a single oral 1.5‐mg dose of tivozanib. Tivozanib was well tolerated in both studies. Steady‐state ketoconazole did not cause a clinically significant change in the pharmacokinetics of a single dose of tivozanib; therefore, dosing of tivozanib with a CYP3A4 pathway inhibitor should not cause a clinically significant change in serum tivozanib levels. However, coadministration of tivozanib with rifampin caused a significant decrease in the area under the curve from 0 to infinity and half‐life and an increase in clearance of tivozanib, which suggest increased clearance via the enhanced CYP3A4‐mediated metabolism of tivozanib.
Relative bioavailability and the effect of meal type and timing on the pharmacokinetics of migalastat in healthy volunteers
Authors: Johnson Franklin K. , Mudd Paul N. , Janmohamed Salim G. 
Published: July 2014

AbstractMigalastat HCl is an investigational, pharmacological chaperone for mutant α‐galactosidase A, which is responsible for Fabry disease, an X‐linked, lysosomal storage disorder. Two Phase I studies evaluated relative bioavailability, effect of meal type and timing on pharmacokinetics, safety, and tolerability of migalastat HCl in healthy volunteers. Study 1 (N = 15, 19–55 years): single 100‐mg doses of migalastat HCl capsule and solution formulations were bioequivalent. The ratios of LSM (90% CIs) for Cmax were 97.1% (86.8–109) and AUC0‐inf 97.9% (88.8–108) under fasted conditions. Single 100‐mg doses of migalastat HCl capsules administered with a high‐fat meal decreased Cmax by 40% and AUC0‐inf by 37%. A high‐fat meal delayed tmax by approximately 1 hour. Study 2 (N = 20, 18–65 years): A high‐fat or light meal up to 1 hour before or after administration of single 150 mg doses of migalastat HCl capsules decreased Cmax and AUC0‐inf up to 40%, but had no apparent effect on tmax (range of medians with food: 1.5–3 hours, median fasted: 3 hours). A 50‐g glucose drink co‐administered with migalastat HCL did not result in clinically significant changes in migalastat absorption. No serious safety or tolerability issues were identified.
Real‐time multiview human pose tracking using graphics processing unit‐accelerated particle swarm optimization
Authors: Rymut Boguslaw , Kwolek Bogdan 
Published: July 2014

SummaryThis paper describes how to achieve real‐time tracking of 3D human motion using multiview images and graphics processing unit (GPU)‐accelerated particle swarm optimization. The tracking involves configuring the 3D human model in the pose described by each particle and then rasterizing it in each 2D plane. The Compute Unified Device Architecture threads rasterize the columns of the triangles and perform the summing of the fitness values of pixels belonging to the processed columns. Such a parallel particle swarm optimization (PSO) exhibits the level of parallelism that allows us to effectively utilize the GPU resources. Image acquisition and image processing are multithreaded and run on CPU in parallel with PSO‐based searching for the best pose. Owing to such task decomposition, the tracking of the full human body can be performed at rates of 12 frames per second. For a PSO consisting of 1000 particles and executing 10 iterations, the GPU achieves an average speedup of 12 over the CPU. Using marker‐less motion capture system consisting of four calibrated and synchronized cameras, the efficiency comparisons were conducted on four CPU cores and four GTX GPUs on two cards. Copyright © 2014 John Wiley & Sons, Ltd.
Capturing the sensitivity of optical network quality metrics to its network interface parameters
Authors: Ortín‐Obón Marta , Ramini Luca , Viñals Víctor , Bertozzi Davide 
Published: July 2014

SUMMARYOptical networks‐on‐chip (ONoCs) are gaining momentum as a way to improve energy consumption and bandwidth scalability in the next generation multicore and many‐core systems. Although many valuable research works have investigated their properties, the vast majority of them lack an accurate exploration of the network interface architecture required to support optical communications on the silicon chip. The complexity of this architecture is especially critical for a specific kind of ONoCs: the wavelength‐routed ones. These are capable of delivering contention‐free all‐to‐all connectivity without the need for path reservation, unlike space‐routed ONoCs. From a logical viewpoint, they can be considered as full nonblocking crossbars; thus, the control complexity is implemented at the network interfaces. To our knowledge, this paper proposes the first complete network interface architecture for wavelength‐routed optical NoCs, by coping with the intricacy of networking issues such as flow control, buffering strategy, deadlock avoidance, serialization, and above all, their codesign in a complete architecture. The evaluation methodology spans from area and energy analysis via actual synthesis runs in 40‐nm technology to RTL‐equivalent (register‐transfer level) SystemC modelling of the network architecture and aims at verifying whether the projected benefits of ONoCs versus their electrical counterparts are still preserved when the complexity of their network interface is considered in the analysis. Copyright © 2014 John Wiley & Sons, Ltd.
Recent Progress in Research on High‐Voltage Electrolytes for Lithium‐Ion Batteries
Authors: Tan Shi , Ji Ya J. , Zhang Zhong R. , Yang Yong 
Published: July 2014

AbstractDeveloping a stable and safe electrolyte that works at voltages as high as 5 V is a formidable challenge in present Li‐ion‐battery research because such high voltages are beyond the electrochemical stability of the conventional carbonate‐based solvents available. In the past few years, extensive efforts have been carried out by the research community toward the exploration of high‐voltage electrolytes. In this review, recent progress in the study of several promising high‐voltage electrolyte systems, as well as their recipes, electrochemical performance, electrode compatibility, and characterization methods, are summarized and reviewed. These new electrolyte systems include high‐voltage film‐forming additives and new solvents, such as sulfones, ionic liquids, nitriles, and fluorinated carbonates. It appears to be very difficult to find a good high‐voltage (∼5 V) electrolyte with a single‐component solvent at the present stage. Using mixed fluorinated–carbonate solvents and additives are two realistic solutions for practical applications in the near term, while sulfones, nitriles, ionic liquids and solid‐state electrolyte/polymer electrolytes are promising candidates for the next generation of high‐voltage electrolyte systems.
An active‐clamping zero‐voltage‐switching flyback converter with integrated transformer
Authors: Lin Jing‐Yuan , Wang Chao‐Fu , Lin Chien‐Yu , Chen John L , Wang Jian‐Min 
Published: July 2014

SummaryThis paper proposes an active‐clamping flyback converter using an integrated transformer. The proposed converter is composed of two active‐clamp flyback converters. The presented converter can balance the total load current between secondary sides of two transformers so that the rectifier diode conduction loss is reduced. Also, the main switch of one converter is the auxiliary switch for the other converter, so that only two switches are required and both can achieve zero‐voltage‐switching operation. The two transformers are integrated into one magnetic core; therefore, the volume and copper loss of transformer can be reduced. Detailed analysis and design of this integrated magnetic active‐clamping flyback converter are described. Experimental results are recorded for a prototype converter with an AC input voltage ranging from 85 to 135 V, an output voltage of 24 V and an output current of 5 A, operating at a switching frequency of 100 kHz. Copyright © 2014 John Wiley & Sons, Ltd.
An analysis of energy consumption for TCP data transfer with burst transmission over a wireless LAN
Authors: Hashimoto Masafumi , Hasegawa Go , Murata Masayuki 
Published: July 2014

SummaryA common strategy for energy saving in wireless network devices is to remain in sleep mode for as long as possible. The timing of packet transmission and reception depends on the behavior of the transport‐layer protocols used by upper‐layer applications. Therefore, understanding the relation between the behavior of the transport‐layer protocols and energy efficiency using sleep mode is important for effective energy saving, especially when a wireless network interface (WNI) is activated in sleep mode at packet interarrivals. In this paper, we analyze the energy consumption of a client's WNI in Transmission Control Protocol (TCP) data transfer over a wireless LAN by focusing on the detailed behavior of TCP congestion control mechanisms. This model considers three situations: the WNI is activated in continuously active mode, in sleep mode, and in sleep mode with burst transmission. The latter is proposed as an effective method to improve energy efficiency, which lengthens sleep periods by transmitting and receiving multiple packets in a bursty fashion. Through numerical examples, we show that sleeping without modification of transmission timing reduces energy consumption in TCP data transfer by only around 10%, and that the burst transmission can contribute further 50% energy reduction. Copyright © 2014 John Wiley & Sons, Ltd.
Sexual and asexual reproduction in the colonial ascidian Botryllus schlosseri
Authors: Gasparini Fabio , Manni Lucia , Cima Francesca , Zaniolo Giovanna , Burighel Paolo , Caicci Federico , Franchi Nicola , Schiavon Filippo , Rigon Francesca , Campagna Davide , Ballarin Loriano 
Published: July 2014

SummaryThe colonial tunicate Botryllus schlosseri is a widespread filter‐feeding ascidian that lives in shallow waters and is easily reared in aquaria. Its peculiar blastogenetic cycle, characterized by the presence of three blastogenetic generations (filtering adults, buds, and budlets) and by recurrent generation changes, has resulted in over 60 years of studies aimed at understanding how sexual and asexual reproduction are coordinated and regulated in the colony. The possibility of using different methodological approaches, from classical genetics to cell transplantation, contributed to the development of this species as a valuable model organism for the study of a variety of biological processes. Here, we review the main studies detailing rearing, staging methods, reproduction and colony growth of this species, emphasizing the asymmetry in sexual and asexual reproduction potential, sexual reproduction in the field and the laboratory, and self‐ and cross‐fertilization. These data, opportunely matched with recent tanscriptomic and genomic outcomes, can give a valuable help to the elucidation of some important steps in chordate evolution. genesis 53:105–120, 2015. © 2014 Wiley Periodicals, Inc.
Iminobisphosphines to (Non‐)Symmetrical Diphosphinoamine Ligands: Metal‐Induced Synthesis of Diphosphorus Nickel Complexes and Application in Ethylene Oligomerisation Reactions
Authors: Boulens Pierre , Lutz Martin , Jeanneau Erwann , Olivier‐Bourbigou Hélène , Reek Joost N. H. , Breuil Pierre‐Alain R. 
Published: July 2014

AbstractWe describe the synthesis of a range of novel iminobisphosphine ligands based on a sulfonamido moiety [R1SO2N=P(R2)2‐P(R3)2]. These molecules rearrange in the presence of nickel by metal‐induced breakage of the P–P bond to yield symmetrical and nonsymmetrical diphosphinoamine nickel complexes of general formula Ni{[P(R2)2]N(SO2R1)P(R3)2}Br2. The complexes can be isolated and are very stable. Upon activation by MAO, these complexes oligomerise ethylene to small chain oligomers (mainly C4–C8) with high productivity. Surprisingly fast codimerisation reactions of ethylene with butenes is observed, leading to a high content of branched C6 products.
Phytochemical contents and oxidative stability of oils from non‐traditional sources
Authors: Hassanien Minar M. M. , Abdel‐Razek Adel G. , Rudzińska Magdalena , Siger Aleksander , Ratusz Katarzyna , Przybylski Roman 
Published: July 2014

Non‐traditional plant oils, such as cold pressed black cumin (Nigella sativa) seeds oil and oils extracted by n‐hexane in the lab conditions from food industry by‐products, namely, apricot kernels (Prunus armeniaca), wheat germ (Triticum vulgare), grape seeds (Vitis vinifera), and tomato seeds (Lycopersicon esculentum) were investigated. Bioactive compounds such as phytosterols, tocopherols, and tocotrienols, and also fatty acid composition were determined by GLC and HPLC. The oxidative stability index of oils was evaluated by rancimat method. The fatty acid composition of lipids from apricot kernels was different from the other oils. The contribution of oleic acid in apricot oil amount 66.77%, while in the other oils ranged from 12.39% to 21.86%. The highest level of α‐linolenic acid was determined in wheat germ oil (7.58%). Concerning phytosterols, β‐sitosterol was major component in all oils extracted from non‐traditional sources, with wheat germ oil being the richest in total phytosterol content. Wheat germ oil was very rich in campesterol and sitostanol. It was found that wheat germ, black cumin seed, tomato seed, and apricot kernel oils contained significant amount of citrostadienol. Concerning the vitamin E, it was found that black cumin seed oil contained highest amount of tocotrienols and gamma tocopherols, while, tomato seed oil contain highest amount of gamma‐tocotrienols. Wheat germ oil was unique in having a high content of alpha‐tocopherol. Apricot kernel and wheat germ oils showed the highest oxidative stability as shown from its induction period compared to the other investigated oils. It is recommended that these oils can be utilized as sources of value added products, natural antioxidants, edible, and healthy oils.Apricot kernels, black cumin, grape, and tomato seeds and wheat germ oils were investigated. Bioactive compounds such as phytosterols, tocopherols, and tocotrienols, and also fatty acid composition were determined by GLC and HPLC. The oxidative stability index of oils was evaluated by rancimat method. It is recommended that these oils can be utilized as sources of value added products, natural antioxidants, edible and healthy oils.
Determination of the Stereostructure of Pyrimidine Nucleoside Derivatives with a Combination of Various Chiroptical Methods
Authors: Górecki Marcin , Karczmarska‐Wódzka Aleksandra , Kołodziejska Renata , Dramiński Marcin , Frelek Jadwiga 
Published: July 2014

AbstractThe absolute configuration of pyrimidine nucleoside derivatives prepared by enantioselective reduction was determined using a combination of electronic circular dichroism (ECD) and vibrational circular dichroism (VCD) spectroscopy in tandem with quantum chemical calculations. Such a combined approach based on a comparison of experimentally measured and theoretically simulated chiroptical properties allows reliable predictions of absolute configuration. The advantage of using more than one chiroptical method for the assignment of absolute configuration is demonstrated. The reliability of the proposed assignment was further confirmed by ECD measurements at variable temperatures and the use of Moscowitz procedure. This allowed the relative energies of the conformers obtained from the calculations to be verified, and the distribution of conformers to be estimated.
Synthesis, Electrochemistry, Crystal Structures, and Optical Properties of Quinoline Derivatives with a 2,2′‐Bithiophene Motif
Authors: Slodek Aneta , Filapek Michal , Szafraniec Grazyna , Grudzka Iwona , Pisarski Wojciech Andrzej , Malecki Jan Grzegorz , Zur Lidia , Grela Malgorzata , Danikiewicz Witold , Krompiec Stanislaw 
Published: July 2014

AbstractNew quinolines bearing a 2,2′‐bithiophene motif have been prepared through Ru‐ and In‐catalyzed reactions as well as by Suzuki cross‐coupling reactions. The novel quinolines have been characterized by using EI‐HRMS and NMR spectroscopy. Additionally, the molecular structures of the novel quinolines were confirmed by X‐ray crystallography. The photophysical and electrochemical properties of all quinoline derivatives were investigated by using absorption and luminescence spectroscopy and cyclic voltammetry. The main intense absorption bands associated with the quinoline derivatives were located between 350 and 450 nm. Intense blue‐green and orange‐red fluorescence, moderate Stokes shifts, and microsecond lifetimes were observed. Quinolines containing one bithiophene moiety underwent oxidation leading to dimerization, whereas bis(bithiophenyl)‐substituted quinoline underwent polymerization. All the studied quinolines showed multistep reversible reduction, with 6‐nitro‐4‐phenylquinoline being the easiest to reduce. The study of novel quinoline derivatives indicates a strong correlation between their electrochemical and spectroscopic properties and the character of the substituent (electron‐donating or electron‐withdrawing) in the quinoline ring.
Synthesis and Cytotoxic Activity of a Small Naphthoquinone Library: First Synthesis of Juglonbutin
Authors: Brötz Elke , Herrmann Jennifer , Wiese Jutta , Zinecker Heidi , Maier Armin , Kelter Gerhardt , Imhoff Johannes F. , Müller Rolf , Paululat Thomas 
Published: July 2014

AbstractA synthetic protocol has been designed to synthesize grecoketidone (2k), 5‐hydroxylapachol (2g), and the recently discovered natural products juglonbutin (2o) and its derivatives, leading to a small library of different 1,4‐naphthoquinones with the intention of finding new active compounds. Within our collection, 2‐O‐alkylated naphthoquinones with an ester functionality in the side‐chain and a free OH group at C‐5 showed the best activities. Compounds 2f, 2m, and 2n showed GI50 values against 12 tumor cell lines in the lower micromolar range and juglonbutin (2o) showed remarkably efficient inhibition of the glycogen synthase kinase 3β with an IC50 value of 2.03 μM. Furthermore, studies on the mode of action of the most active cytotoxic compounds have been carried out. To the best of our knowledge, this is the first report on the synthesis of juglonbutin (2o) and its biological activity.
One‐Pot Preparation of Enantiopure Fluorinated β‐Amino Acid Precursors
Authors: Jones Joshua H. , Appayee Chandrakumar , Brenner‐Moyer Stacey E. 
Published: July 2014

AbstractChiral β‐fluoro amines and β,β‐difluoro amines are common substructures in medicinal compounds. Industrial syntheses typically use enantiopure starting materials, chiral auxiliaries, or the resolution of enantiomeric or diastereomeric mixtures to install these functionalities in enantiopure form. With the goal of improving access to these substructures, we recently developed the first catalytic enantioselective olefin aminohalogenation reaction, which produced chiral β‐fluoro amines in a single flask from achiral enal starting materials. This paper describes the extension of this method to the preparation of β‐amino‐α,α‐difluoro carbonyl compounds. Specifically, carbon–nitrogen and carbon–fluorine bond‐forming reactions were combined in an organocascade reaction to produce β‐amino‐α,α‐difluoro carbonyl compounds containing alkyl substituents at the β‐position. As such, this method is mechanistically distinct from, and complementary to, existing one‐pot catalytic enantioselective methods for the preparation of fluorinated β‐amino acid precursors.
Boron/Zinc Exchange Reaction in the Diastereoselective Arylation of N‐Protected L‐Prolinal
Authors: Martins Bruna S. , Lüdtke Diogo S. 
Published: July 2014

AbstractThe diastereoselective arylation of chiral, non‐racemic, N‐trityl‐protected L‐prolinal has been investigated. The reactive aryl groups were generated by a boron/zinc exchange reaction between arylboronic acids and diethylzinc. The reactions proceeded in a highly diastereoselective fashion, and the resulting amino alcohols possessing two vicinal stereocenters were obtained in diastereomeric ratios of >20:1, regardless of the substituent at the transferable aryl group. The diastereoselectivity of the reactions is believed to be the result of an energetically favored Felkin–Anh transition state, with the competing Cram‐chelation pathway precluded due to the presence of the bulky N‐trityl protecting group.
Stereoselective Synthesis of Enantiopure Oxetanes, a Carbohydrate Mimic, an ϵ‐Lactone, and Cyclitols from Biocatalytically Derived β‐Hydroxy Esters as Chiral Precursors
Authors: Das Debabrata , Halder Joydev , Bhuniya Rajib , Nanda Samik 
Published: July 2014

AbstractBiocatalytically derived enantiopure α‐substituted β‐hydroxy esters serve as excellent chirons for the synthesis of a diverse set of structures such as oxetanes, a carbohydrate mimic, an ϵ‐lactone, and carbocyclic and aromatic cyclitols. The starting materials can be easily accessed in enantiopure form from α‐substituted β‐keto esters by biocatalytic reduction with Klebsiella pneumoniae (NBRC 3319). Ring‐closing metathesis (RCM) is one of the key transformations used to create the carbocyclic/heterocyclic frameworks reported in this article. The synthesized cyclitols were screened for their inhibitory effect on α‐ and β‐glucosidases.
Dynamic frequency management in 802.11‐based multi‐radio wireless networks
Authors: Athanasiou George , Tassiulas Leandros 
Published: July 2014

ABSTRACTEfficient channel selection is essential in 802.11 mesh deployments, for minimising contention and interference among co‐channel devices and thereby supporting a plurality of quality of service (QoS)‐sensitive applications. A few protocols have been proposed for frequency allocation in such networks; however, they do not address the problem end‐to‐end. In this paper, we present a general formulation of the channel selection problem, taking into account the performance of both mesh access and mesh backhaul. Moreover, we propose a routing‐aware channel selection protocol for wireless mesh networks (ARACHNE). ARACHNE is distributed in nature and motivated by our measurements on a wireless testbed. The main novelty of our protocol comes from adopting a metric that captures the end‐to‐end link loads across different routes in the network. ARACHNE prioritises the assignment of low‐interference channels to links that (i) need to serve high‐load aggregate traffic and/or (ii) already suffer significant levels of contention and interference. Our protocol takes into account the number of potential interfaces (radios) per device and allocates these interfaces in a manner that efficiently utilises the available channel capacity. We evaluate ARACHNE through extensive, trace‐driven simulations, and we show the approaches to the optimal channel selection. We observe that our protocol improves the total network throughput, as compared to three other representative channel allocation approaches in literature. Copyright © 2014 John Wiley & Sons, Ltd.