bluuebunny/crossref_metadata_2025_split huggingface dataset:
Synthesis and biological evaluation of some heterocyclic scaffolds based on the multifunctional N‐(4‐acetylphenyl)‐2‐chloroacetamide
Authors: Abdel‐Latif Ehab , Fahad Mustafa M. , El‐Demerdash Amr , Ismail Mohamed A. 
Published: May 2020

AbstractThe chloroacetamide derivative, 1, was used as a versatile precursor for the synthesis of various types of N‐aryl‐2‐(benzothiazol‐2‐ylthio)acetamide derivatives. The reaction of 1 with 2‐mercaptobenzothiazole followed by condensation reaction of the produced sulfide with phenylhydrazine, 2‐cyanoacetohydrazide, and/or thiosemicarbazide furnished the conforming condensation products, 4, 7, and 10, respectively. Treatment of the phenylhydrazone product, 4, with Vilsmeier formylation reagent (POCl3/DMF) yielded the corresponding 4‐formylpyrazole derivative, 5. The thiosemicarbazone product, 10, was reacted with ethyl bromoacetate to furnish the thiazolin‐4‐one derivative, 11. The substitution reactions of chloroacetamide derivative, 1, with 2‐mercapto‐4,6‐dimethylnicotinonitrile and 6‐amino‐2‐mercaptopyrimidin‐4‐ol, were explored to identify the sulfide products, 14 and 17. Cyclization of 14 into its corresponding thieno[2,3‐b]pyridine compound, 15, was performed using sodium ethoxide. The thiosemicarbazone, 10, and sulfide derivative, 14, were found to be the most potent antibacterial compounds against Escherichia coli and Staphylococcus aureus, exhibiting growth inhibitory activities of 80.8% and 91.7%, respectively. Moreover, the thiosemicarbazone, 10, displayed the most significant antioxidant activity with inhibitory activity of 82.6%, which comes close to the antioxidant activity of L‐ascorbic acid.
Zinc and cadmium complexation of L‐methionine: An infrared multiple photon dissociation spectroscopy and theoretical study
Authors: Boles Georgia C. , Stevenson Brandon C. , Hightower Randy L. , Berden Giel , Oomens Jos , Armentrout P. B. 
Published: May 2020

AbstractMethionine (Met) cationized with Zn2+, forming Zn (Met–H)+(ACN) where ACN = acetonitrile, Zn (Met–H)+, and ZnCl+(Met), as well as Cd2+, forming CdCl+(Met), were examined by infrared multiple photon dissociation (IRMPD) action spectroscopy using light generated from the FELIX free electron laser. A series of low‐energy conformers for each complex was found using quantum‐chemical calculations in order to identify the structures formed experimentally. For all four complexes, spectral comparison indicated that the main binding motif observed is a charge solvated, tridentate structure where the metal center binds to the backbone amino group nitrogen, backbone carbonyl oxygen (where the carboxylic acid is deprotonated in two of the Zn2+ complexes), and side‐chain sulfur. For all species, the predicted ground structures reproduce the experimental spectra well, although low‐lying conformers characterized by similar binding motifs may also contribute in each system. The current work provides valuable information regarding the binding interaction between Met and biologically relevant metals. Further, the comparison between the current work and previous analyses involving alkali metal cationized Met as well as cysteine (the other sulfur containing amino acid) cationized with Zn2+ and Cd2+ allows for the elucidation of important metal dependent trends associated with physiologically important metal–sulfur binding.
New marsupialization technique in endolymphatic sac surgery
Authors: Daneshi Ahmad , Hosseinzadeh Farideh , Mohebbi Saleh , Mohseni Mohammad , Mohammadi S. Saeed , Asghari Alimohamad 
Published: May 2020

AbstractObjectivesThe aim of the present study was to describe and evaluate the results of a new technique in endolymphatic sac decompression surgery.MethodsForty‐three patients with intractable unilateral Meniere's disease were selected. Endolymphatic sac was identified after simple mastoidectomy, and its lateral layer was incised, using a sickle knife. Outer layer of the sac was turned around and placed under the anterior bony border.ResultsMean duration of the follow‐up was 24 months. Mean tinnitus handicap index, pure tone average (PTA) on thresholds at 500, 1000, 2000, and 4000 Hz, mean speech reception threshold, mean speech discrimination score, hearing stage, and mean vertigo score before and after surgery were evaluated.ConclusionThe new marsupialization technique with anterior bony border is a safe and effective way to improve tinnitus, vertigo, and ear fullness among these patients. According to PTA and hearing stage, this surgery can control progressive hearing loss.Level of Evidence3
Congenital toxoplasmosis: What is the evidence for chemoprophylaxis to prevent fetal infection?
Authors: Mandelbrot Laurent 
Published: May 2020

AbstractAlthough prenatal diagnosis and prenatal and neonatal therapy of congenital toxoplasmosis are available, there is controversy concerning the effectiveness of prophylaxis to prevent placental transmission. Experimental, parasitological, and clinical data suggest a “window of opportunity” following maternal infection. Among medications active against Toxoplasma gondii, mainly spiramycin (Spy) and pyrimethamine + sulfonamide combinations (P‐S) have been evaluated. Results from observational studies suffered treatment bias, since prescriptions differed according to the gestational age at seroconversion, which is the major risk factor for transmission, and many lacked precise timing. Some large retrospective studies found no difference in transmission according to prophylactic treatment, but transmission was lower when treatment started promptly after maternal seroconversion. A few recent studies adjusting for timing of infection observed lower transmission in case of P‐S than other or no prophylaxis. In the only randomized controlled trial, transmission was lower with P‐S than S (18.5% vs 30%, P = .147); this association was strengthened when the treatment was started within 3 weeks of seroconversion, and the incidence of fetal cerebral ultrasound signs was significantly reduced in the P‐S group. Rapid initiation of prophylactic therapy following maternal infection, which is usually asymptomatic, requires systematic screening for maternal seroconversion during pregnancy.
Cyclic polymers: Advances in their synthesis, properties, and biomedical applications
Authors: Liénard Romain , De Winter Julien , Coulembier Olivier 
Published: May 2020

AbstractSince the time first synthetic macrocycles were observed as academic curiosities, great advances have been made. Thanks to the development of controlled polymerization processes, new catalytic systems and characterization techniques during the last decades, well‐defined cyclic polymers are now readily accessible. This further permits the determination of their unique set of properties, mainly due to their lack of chain ends, and their use for industrial applications can now be foreshadowed. This review aims to give an overview on the recent progresses in the field of ring polymers to this day. The current state of the art of the preparation of cyclic polymers, the challenges related to it such as the purification of the samples and the scalability of the synthetic processes, the properties arising from the cyclic topology and the potential use of cyclo‐based polymers for biomedical applications are as many topics covered in this review.
Exercise testing for children with cystic fibrosis: A systematic review
Authors: Lang Ray Lei , Stockton Kellie , Wilson Christine , Russell Trevor Glen , Johnston Leanne Marie 
Published: May 2020

AbstractBackgroundExercise testing is routinely used to measure exercise capacity in children with cystic fibrosis (CF). Various tests are available, however the psychometric properties of these measures have not been systematically reviewed for this population.MethodA systematic search of electronic databases (PubMed, Web of Science, Medline, CINHAL, Cochrane, and PEDro) was performed to identify papers that: (a) reported original psychometric data, (b) examined a measure of exercise capacity, (c) examined children with CF aged eight to 18 years; and (d) were published in English after 1950. The level of psychometric evidence was evaluated using the COnsensus‐based Standards for the selection of health Measurement INstruments (COSMIN) checklist.ResultsSearches identified 1025 papers. Forty‐six papers were included, covering 15 tests: incremental cardiopulmonary exercise test using a cycle ergometer (CPET(cycle)) or treadmill (CPET(treadmill)), 6 minute walk test (6MWT), modified shuttle test (MST), 3‐minute step test (3MST), 2 minute walk test (2MWT), Bratteby walk test, intermittent sprint test, speed ramp test, incremental step test, forward‐backwards jump test (FBJT), astride jump test (AJT), motor quotient test, Munich fitness test, and Glittre ADL test.ConclusionThere is a plethora of exercise tests available with varying psychometric robustness. The CPET, 6MWT, and MST have fair to good psychometric properties, but each with their clinical advantages and limitations. Thus, a Selection Guide was developed to assist clinicians and researchers in selecting the most appropriate exercise test for various situations.
Trypsin inhibitor from Enterolobium contortisiliquum seeds impairs Aedes aegypti development and enhances the activity of Bacillus thuringiensis toxins
Authors: Tabosa Pedro M S , Almeida Filho Luiz C P , Franca Rute X , Rocha‐Bezerra Lady Clarissa B , Vasconcelos Ilka M , Carvalho Ana F U 
Published: May 2020

AbstractBACKGROUNDDisease vector insects are barriers for human development. The use of synthetic chemicals to control these vectors has caused damage to the environment and contributed to the arising of resistant insect populations. This has led to an increased search for plant‐derived molecules with insecticidal activity or that show synergistic effects with known insecticidal substances, such as protease inhibitors. Thus, we aimed to evaluate the effect of Enterolobium contortisiliquum trypsin inhibitor (EcTI) on Aedes aegypti development as well as its effect on insecticidal activity of Bacillus thuringiensis toxins.RESULTSEcTI showed an apparent molecular mass about of 20 kDa in SDS‐PAGE and was able to inhibit in vitro the activity of trypsin and proteases from midgut of Ae. aegypti larvae. EcTI was not able to cause acute toxicity on mosquito larvae even at 1000 μg mL−1, however it promoted a delay in larval development after prolonged exposure. The zymogram results for EcTI‐treated larvae (from 50 to 200 μg mL−1) showed an increase of midgut proteases activity as a larvae defense mechanism, however no changes in the enzyme profile was observed. These same concentrations were able to enhance up to three fold the insecticidal activity of B. thuringiensis toxins without causing toxicity to Artemia sp. nauplii, a non‐target organism.CONCLUSIONSThe results offer a novel approach by combining EcTI and B. thuringiensis toxins for combating Ae. aegypti larvae. © 2020 Society of Chemical Industry
Metribuzin resistance via enhanced metabolism in a multiple herbicide resistant Lolium rigidum population
Authors: Ma Hongju , Lu Huan , Han Heping , Yu Qin , Powles Stephen 
Published: May 2020

AbstractBACKGROUNDThe photosystem II (PSII)‐inhibiting herbicides are important for Australian farmers to control Lolium rigidum Gaud. and other weed species in trazine tolerant (TT)‐canola fields. A L. rigidum population (R) collected from a TT‐canola field from Western Australia showed multiple resistance to PSII, acetyl‐coenzyme A carboxylase (ACCase) and acetolactate synthase (ALS) inhibitors. The mechanisms of multiple resistance in this R population were determined.RESULTSThe R population showed a low‐level (about 3.0‐fold) resistance to the PSII‐inhibiting herbicides metribuzin and atrazine. Sequencing of the psbA gene revealed no differences between the R and susceptible (S) sequences. Furthermore, [14C]‐metribuzin experiments found no significant difference in metribuzin foliar uptake and translocation between the R and S plants. However, [14C]‐metribuzin metabolism in R plants was 2.3‐fold greater than in S plants. The cytochrome P450 monooxygenase inhibitor piperonyl butoxide (PBO) enhanced plant mortality response to metribuzin and atrazine in both R and S populations. In addition, multiple resistance to ALS and ACCase inhibitors are due to known resistance mutations in ALS and ACCase genes.CONCLUSIONThe results demonstrate that enhanced metribuzin metabolism likely involving cytochrome P450 monooxygenase contributes to metribuzin resistance in Lolium rigidum. This is the first report of metabolic resistance to the PSII‐inhibiting herbicide metribuzin in Australian Lolium rigidum. © 2020 Society of Chemical Industry
Construction of Strandberg‐Type Polyoxometalate‐Based Inorganic‐Organic Hybrid Material with Water‐Assisted Proton Conductivity
Authors: Wang Jia–Xuan , Liang Song , Tan Huaqiao , Wang Yong–Hui , Zang Hong–Ying , Li Yang–Guang 
Published: May 2020

AbstractPolyoxometalates (POMs) were widely applied in the field of proton conduction due to their rapid charge transfer capability and large proton capacity. The Strandberg‐type POM has small size and large charge density, can form functional organometallic compounds with metal ions. In this study, by using [P2Mo5O23]6− coordinate with the cobalt ion with cytosine as the structure‐directing agent, a compound of Co1.5(C4H6N3O)3[P2Mo5O23]⋅8.5H2O was synthesized, which showed one‐dimensional chain structure and exhibits proton conductivity of 3.62 × 10−4 S cm−1 at 98 °C and 97% RH. The amino group and nitrogen atoms in the cytosine can form hydrogen bond with the coordination water molecules. Meanwhile, the hydrogen bond network can also be formed between the water molecules, which is one of the main factors for proton conduction performance. The compound Co1.5(C4H6N3O)3[P2Mo5O23]⋅8.5H2O exhibited the corresponding activation energies and conduction mechanisms at different temperature intervals, by analyzing the temperature‐dependent PXRD spectrum under high‐humidity conditions, which showed the hydrogen bond network of the crystal during the temperature changes affects its proton conduction performance.
Phosphoric Acid Functionalized Nanostructured Heterogeneous Catalyst for Multicomponent Synthesis of 2‐Amino‐4H‐chromene
Authors: Kalita Priyanka , Rani Das Doli , Kumar Talukdar Anup 
Published: May 2020

AbstractFunctionalization of synthesized mesoporous MCM‐48 was performed using phosphoric acid via post synthesis modification method and characterized using different analytical techniques. The acidic character of the phosphoric acid modified material was enhanced compared to parent MCM‐48 as predicted from the Ammonia‐Temperature Programmed Desorption (NH3‐TPD) analysis. The catalytic activity of the synthesized materials was investigated for the synthesis of 2‐amino‐4H‐chromene via one pot three component reaction using aldehyde, malononitrile and dimedone using ethanol as solvent at 60 °C. Moderate to good yields of the desired products were obtained with substituted benzaldehyde under the optimized reaction condition. Moreover, reusability of the catalyst was also demonstrated upto five catalytic cycles with minimal loss in catalytic activity.
Noscapine‐Loaded Nanostructured Lipid Carriers as a Potential Topical Delivery to Bovine Mastitis Treatment
Authors: Otarola Jessica J. , Alejandra Luna Maria , Mariano Correa Néstor , Molina Patricia G. 
Published: May 2020

AbstractNoscapine (NO) is a lipophilic benzylisoquinoline alkaloid with antioxidant, antitussive and anti‐cancer properties. This study aimed to incorporate this alkaloid into an innovative topical gel‐based on nanostructured lipid carrier (NLCs) to facilitate its incorporation and distribution into the organism to bovine mastitis treatment.Drug release studies were carried out using square wave voltammetry (SWV) as an alternative technique. The NLCs showed a 100 % encapsulation efficiency and, a fast release profile, releasing 86.7 % of the incorporated NO in 5 hours.On the other hand, the lipid nanoparticles′ stability was analyzed using SWV and transmission electron microscope techniques. For these studies, NLCs with and without NO incorporated were immobilized onto a carbon paste electrode and exposed to free radicals attack. The stability studies were assisted with dynamic light scattering.The results reveal a promising alternative drug delivery system for NO topical application.
Design, Synthesis and Cytotoxic Activities of Pyrazole‐Perimidine Hybrids
Authors: Gümüş Mehmet , Gümüş Nisa , Eroğlu Halil Erhan , Koca İrfan 
Published: May 2020

AbstractThe hybrid molecules are one of the powerful tools used in the new drug discovery. In this work, nine perimidine‐pyrazole hybrids were designed and synthesized. All structures of the novel compounds were characterized elemental analysis, FTIR, NMR and HRMS. Genotoxic, mutagenic and carcinogenic effects of two of the synthesized compounds were evaluated. The tested compounds could cause chromosomal damage by genotoxic potential and mitotic delay by cytotoxic potential at high concentrations (25‐100 μM).
Electrochemically Induced Facile and Efficient Multicomponent Approach to Medicinally Relevant 4‐[4‐oxo‐4H‐pyran‐2‐yl](aryl)‐methylisoxazol‐5(2H)‐one Scaffold
Authors: Elinson Michail N. , Ryzhkova Yuliya E. , Ryzhkov Fedor V. , Vereshchagin Anatoly N. , Leonova Natalia A. , Egorov Mikhail P. 
Published: May 2020

AbstractThe new electrochemically induced multicomponent assembling has been accomplished: the electrocatalytic transformation of aldehydes, 3‐aryl‐substituted isoxazol‐5(4H)‐ones and kojic acid has been carried out in alcohols in an undivided cellin the presence of sodium halides. This transformation proceeds with the selective formation of the earlier unknown substituted 4‐{[3‐hydroxy‐6‐(hydroxymethyl)‐4‐oxo‐4H‐pyran‐2‐yl]‐(aryl)methyl}‐isoxazol‐5(2H)‐ones in 57–93 % yields with 190–310 % current efficiency. This new electrocatalytic process provides a facile and efficient way to the separated by C‐aryl‐substituted spacer 3‐arylisoxazol‐5(4H)‐one and kojic acid pharmacology active heterocyclic fragments, which are promising compounds for different biomedical applications, and, in particular, for regulation of inflammatory as was shown by docking studies in this research.
Das Stahldach der BCF‐Arena in Fribourg, Schweiz
Authors: Guscetti Gabriele , Pirazzi Claudio , Degani Nicola , Hess Ivan , Valeiras Oscar , Sottas Solenghi Laure , Gremaud Antoine 
Published: May 2020

AbstractDer folgende Beitrag befasst sich mit der Tragwerkskonzeption sowie mit der Ausführung des Stahldachs der BCF‐Arena im schweizerischen Fribourg. Das Tragwerk überspannt eine Gesamtfläche von etwa 8 500 m2 und wird aus einem Netz sich kreuzender, unterspannter Stahlträger mit veränderlicher Höhe gebildet. Diese verlaufen tangential um den ovalen Zentralring. Ihre geometrische Anordnung folgt dem Prinzip der Spannungstrajektorien. Zur Optimierung der Spanngliedgeometrie kam ein Formfindungsprozess unter Ansatz der dynamischen Relaxation zum Einsatz. Aufgrund der vielen verschiedenen Einflussparameter und in Anbetracht der komplexen Geometrie wurde das Dachtragwerk komplett parametrisch modelliert. Dies ermöglichte die schnelle Studie verschiedener Varianten sowie einen äußerst effizienten Austausch zwischen Geometrie‐ und Rechenmodellen bis hin zur Fabrikation der Einzelkomponenten. Mithilfe dieses Werkzeugs war es möglich, den sehr ambitiösen Terminplan einzuhalten.
Label‐free laser scanning microscopy targeting sentinel lymph node diagnostics: A feasibility study ex vivo
Authors: Kantere Despoina , Siarov Jan , De Lara Shahin , Parhizkar Samad , Olofsson Bagge Roger , Wennberg Larkö Ann‐Marie , Ericson Marica B. 
Published: May 2020

AbstractThis proof‐of‐concept, observational study investigates the potential for label‐free, laser scanning microscopy to identify melanoma metastatic features in lymph node tissues ex vivo ‐ exploring the translational potential targeting sentinel lymph node diagnostics. Ten lymph node samples, of which seven are positive for melanoma metastases and three negative, were obtained from a tissue biobank. Imaging data acquired using multiphoton microscopy ex vivo were compared with histopathological findings. Morphologic features characteristic for histopathologic diagnosis of melanoma metastasis were confirmed in the positive samples. Four of the samples were complementary studied with reflectance mode confocal microscopy; however, visualization was found restricted to fibrous structures in this case. To conclude, the results imply that multiphoton microscopy based on autofluorescence is a promising label‐free technique for visualization of cellular features in lymph node tissues.
Mobility and Migration in Mediterranean Europe: The Case of Agro-pastoralism
Authors: Nori Michele , Farinella Domenica 
Published: May 2020

AbstractWhile most of the existing literature on rural migrations focuses on immigrant workers in intensive agricultural systems, this work tries filling existing gaps by addressing more marginal and remote rural settings. The mountainous, inner and island territories that cover a large part of the Mediterranean are particularly affected by intense demographic decline, land abandonment and problems of generational renewal, posing important questions concerning the sustainability of local development.
Time trends in deaths before age 50 years in people with type 1 diabetes: a nationwide analysis from Scotland 2004–2017
Authors:   for the Scottish Diabetes Research Network Epidemiology Group, O’Reilly Joseph E. , Blackbourn Luke A. K. , Caparrotta Thomas M. , Jeyam Anita , Kennon Brian , Leese Graham P. , Lindsay Robert S. , McCrimmon Rory J. , McGurnaghan Stuart J. , McKeigue Paul M. , McKnight John A. , Petrie John R. , Philip Sam , Sattar Naveed , Wild Sarah H. , Colhoun Helen M. 
Published: May 2020

Abstract
Aims/hypothesis
We aimed to examine whether crude mortality and mortality relative to the general population below 50 years of age have improved in recent years in those with type 1 diabetes.

Methods
Individuals with type 1 diabetes aged below 50 and at least 1 year old at any time between 2004 and 2017 in Scotland were identified using the national register. Death data were obtained by linkage to Scottish national death registrations. Indirect age standardisation was used to calculate sex-specific standardised mortality ratios (SMRs). Poisson regression was used to test for calendar-time effects as incidence rate ratios (IRRs).

Results
There were 1138 deaths in 251,143 person-years among 27,935 people with type 1 diabetes. There was a significant decline in mortality rate over time (IRR for calendar year 0.983 [95% CI 0.967, 0.998], p = 0.03), but the SMR remained approximately stable at 3.1 and 3.6 in men and 4.09 and 4.16 in women for 2004 and 2017, respectively. Diabetic ketoacidosis or coma (DKAoC) accounted for 22% of deaths and the rate did not decline significantly (IRR 0.975 [95% CI 0.94, 1.011], p = 0.168); 79.3% of DKAoC deaths occurred out of hospital. Circulatory diseases accounted for 27% of deaths and did decline significantly (IRR 0.946 [95% CI 0.914, 0.979], p = 0.002).

Conclusions/interpretation
Absolute mortality has fallen, but the relative impact of type 1 diabetes on mortality below 50 years has not improved. There is scope to improve prevention of premature circulatory diseases and DKAoC and to develop more effective strategies for enabling people with type 1 diabetes to avoid clinically significant hyper- or hypoglycaemia.