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Margarida Espadinha, Jorge Dourado, Rocio Lajarin-Cuesta, Clara Herrera-Arozamena, Lidia Gonçalves, Maria Isabel Rodríguez-Franco, Cristobal de Los Rios, Maria M M Santos
N-Methyl-D-aspartate (NMDA) receptors are fundamental for the normal function of the central nerve system, and play an important role in memory and learning. An overactivation of these receptors will lead to neuronal loss associated with major neurological disorders, such as Parkinson's disease, Alzheimer's disease, schizophrenia, and epilepsy. Herein, twenty two novel enantiopure bicyclic lactams were designed, synthesized, and evaluated as NMDA receptor antagonists. Most of the new compounds displayed NMDA receptor antagonism and, the most promising compound showed IC50 value in the same order of magnitude of memantine, a NMDA receptor antagonist used in the clinic for the treatment of Alzheimer's disease...
February 20, 2017: ChemMedChem
Alessandra Monaco, Blanka R Szulc, Zenobia X Rao, Marta Barniol-Xicota, Moussa Sehailia, Bruno Borges, Stephen Hilton
An intramolecular acylal cyclisation (IAC) approach to the synthesis of a range of bicyclic heterocycles is reported. As an example of the utility of the IAC reaction, the methodology was applied in a protecting-group free five-step total synthesis of (±)-lycorane, incorporating a novel intramolecular Heck addition reaction to generate the pentacyclic core structure of the natural product in good yield.
February 19, 2017: Chemistry: a European Journal
Max Wagener, Roger Abächerli, Ursina Honegger, Nicolas Schaerli, Gil Prêtre, Raphael Twerenbold, Christian Puelacher, Germaine Sunier, Philipp Reddiess, Maria Rubini Gimenez, Karin Wildi, Jasper Boeddinghaus, Thomas Nestelberger, Patrick Badertscher, Zaid Sabti, Ramun Schmid, Remo Leber, Dayana Flores Widmer, Samyut Shrestha, Ivo Strebel, Damian Wild, Stefan Osswald, Michael Zellweger, Christian Mueller, Tobias Reichlin
We aimed to assess the diagnostic and prognostic value of ST-segment deviation in aVR, a lead often ignored in clinical practice, during exercise testing and to compare it to the most widely used criterion of ST-segment depression in V5. We enrolled 1,596 patients with suspected myocardial ischemia referred for nuclear perfusion imaging undergoing bicycle stress testing. ST-segment amplitudes in leads aVR and V5 were automatically measured. The presence of inducible myocardial ischemia was the diagnostic end point and adjudicated based on nuclear perfusion imaging and coronary angiography...
January 5, 2017: American Journal of Cardiology
Ben Beck, Christina L Ekegren, Peter Cameron, Mark Stevenson, Rodney Judson, Andrew Bucknill, Elton Edwards, Belinda Gabbe
Accurate coding of injury event information is critical in developing targeted injury prevention strategies. However, little is known about the validity of the most universally used coding system, the International Classification of Diseases (ICD-10), in characterising crash counterparts in pedal cycling events. This study aimed to determine the agreement between hospital-coded ICD-10-AM (Australian modification) external cause codes with self-reported crash characteristics in a sample of pedal cyclists admitted to hospital following bicycle crashes...
February 16, 2017: Injury Prevention: Journal of the International Society for Child and Adolescent Injury Prevention
Caroline Kihlström, Michael Möller, Katarina Lönn, Olof Wolf
BACKGROUND: Large multi-centre studies of clavicle fractures have so far been missing. The aim of this observational study was to describe the epidemiology, classification and treatment of clavicle fractures in the The Swedish Fracture Register (SFR) that collects national prospective data from large fracture populations. METHODS: Data were retrieved from the SFR on all clavicle fractures sustained by patients ≥ 15 years of age in 2013-2014 (n = 2 422) with regards to date of injury, cause of injury, fracture classification and treatment...
February 15, 2017: BMC Musculoskeletal Disorders
Pierre Milbeo, Laure Moulat, Claude Didierjean, Emmanuel Aubert, Jean Martinez, Monique Calmès
The synthesis of enantiopure 1,2-diaminobicyclo[2.2.2]octane (DABO) 1 and its two selectively N-Boc mono-protected derivatives 15 and 16 is described. Starting from bicyclic β-amino acid 3 or 5, strategies involving Curtius and Hofmann rearrangements were explored, demonstrating the unprecedented influence of the bicyclic backbone unsaturation for the preparation of the corresponding diamines that could be only obtained in good yield using the Hofmann rearrangement of unsaturated compound 3. The divergent outcome observed during the Hofmann rearrangement of 3 and 5 was investigated by DFT calculations...
February 15, 2017: Journal of Organic Chemistry
Leonid V Kapilevich, Anna N Zakharova, Anastasia V Kabachkova, Tatyana A Kironenko, Sergei N Orlov
Extensive exercise increases the plasma content of IL-6, IL-8, IL-15, leukemia inhibitory factor (LIF), and several other cytokines via their augmented transcription in skeletal muscle cells. However, the relative impact of aerobic and resistant training interventions on cytokine production remains poorly defined. In this study, we compared effects of dynamic and static load on cytokine plasma content in elite strength- and endurance-trained athletes vs. healthy untrained volunteers. The plasma cytokine content was measured before, immediately after, and 30 min post-exercise using enzyme-linked immunosorbent assay...
2017: Frontiers in Physiology
Jana A Hirsch, Katie A Meyer, Marc Peterson, Le Zhang, Daniel A Rodriguez, Penny Gordon-Larsen
BACKGROUND: We studied the effect of key development and expansion of an off-road multipurpose trail system in Minneapolis, Minnesota between 2000 and 2007 to understand whether infrastructure investments are associated with increases in commuting by bicycle. METHODS: We used repeated measures regression on tract-level (N = 116 tracts) data to examine changes in bicycle commuting between 2000 and 2008-2012. We investigated: 1) trail proximity measured as distance from the trail system and 2) trail potential use measured as the proportion of commuting trips to destinations that might traverse the trail system...
February 13, 2017: International Journal of Behavioral Nutrition and Physical Activity
Gabriele Prati, Luca Pietrantoni, Federico Fraboni
To investigate the factors predicting severity of bicycle crashes in Italy, we used an observational study of official statistics. We applied two of the most widely used data mining techniques, CHAID decision tree technique and Bayesian network analysis. We used data provided by the Italian National Institute of Statistics on road crashes that occurred on the Italian road network during the period ranging from 2011 to 2013. In the present study, the dataset contains information about road crashes occurred on the Italian road network during the period ranging from 2011 to 2013...
February 8, 2017: Accident; Analysis and Prevention
Matthew A Kilgas, Steven J Elmer
We implemented a team-based activity in our exercise physiology teaching laboratory that was inspired from Abbott et al.'s classic 1952 Journal of Physiology paper titled "The physiological cost of negative work." Abbott et al. connected two bicycles via one chain. One person cycled forward (muscle shortening contractions, positive work) while the other resisted the reverse moving pedals (muscle lengthening contractions, negative work), and the cost of work was compared. This study was the first to link human whole body energetics with isolated muscle force-velocity characteristics...
March 1, 2017: Advances in Physiology Education
Fernando Rabasa-Alcañiz, Amparo Asensio, María Sánchez-Roselló, Marcos Escolano, Carlos Del Pozo, Santos Fustero
The intramolecular 1,3-dipolar cycloaddition of ortho-substituted 1,1,1-trifluoromethylstyrene-derived nitrones is described. Tricyclic fused isoxazolidines were obtained as major or exclusive products, in contrast to the case for nonfluorinated substrates, which rendered the bridged derivatives. This change in the regioselectivity was attributed to the electronic and, particularly, steric requirements of the trifluoromethyl group in comparison to the methyl group. It is worth mentioning that trifluoromethylstyrenes have been employed for the first time as dipolarophiles in a 1,3-dipolar intramolecular cycloaddition reaction, leading to the corresponding isoxazolidines bearing a quaternary trifluoromethyl moiety...
February 20, 2017: Journal of Organic Chemistry
Michelle Bezanson, Anna Tomberg, Nicolas Moitessier
We previously reported the synthesis of polysubstituted chiral oxazepanes in three steps from commercially available starting materials. The unexpected reaction of one of these 1,4-oxazepanes in the presence of TBAF provided a 4-oxa-1-azabicyclo[4.1.0]heptane core. This unusual process significantly increased the complexity of the molecular scaffold by introducing a bicyclic core. Surprisingly, the generated bicyclic structure featuring three stereocenters was a mixture of enantiomers with no other diastereomers observed...
February 20, 2017: Journal of Organic Chemistry
Miki Haramura, Yohei Takai, Takaya Yoshimoto, Masayoshi Yamamoto, Hiroaki Kanehisa
BACKGROUND: The purpose of this study was to quantify cardiorespiratory and metabolic responses to body mass-based squat exercise, with specific emphasis on the relationships with the exercise duration. METHODS: Fifteen healthy young men performed body mass-based squat exercise as well as an incremental loaded bicycle test, which determine maximal oxygen uptake and maximal heart rate, with an interval of 2 days between the tests. During both tasks, oxygen uptake, blood lactate concentration (BLa), and heart rate (HR) were determined...
February 8, 2017: Journal of Physiological Anthropology
Song Wei Benjamin Tan, Christina L L Chai, Mark G Moloney
Mono and dihydroxypyrrolidinones are readily available by direct oxygenation of a pyroglutamate-derived bicyclic lactam with high diastereoselectivity, and these may be manipulated further in protected or unprotected form by Grignard addition to a pendant Weinreb amide to give acylhydroxypyrrolidinones, which are analogues of the natural product, pramanicin. Preliminary bioassay against S. aureus and E. coli indicated that some compounds exhibit selective Gram-negative antibacterial activity, and may offer promise for the development of novel systems suitable for antibacterial drug development...
February 7, 2017: Organic & Biomolecular Chemistry
Andrew N Keller, Sidonia B G Eckle, Weijun Xu, Ligong Liu, Victoria A Hughes, Jeffrey Y W Mak, Bronwyn S Meehan, Troi Pediongco, Richard W Birkinshaw, Zhenjun Chen, Huimeng Wang, Criselle D'Souza, Lars Kjer-Nielsen, Nicholas A Gherardin, Dale I Godfrey, Lyudmila Kostenko, Alexandra J Corbett, Anthony W Purcell, David P Fairlie, James McCluskey, Jamie Rossjohn
The major-histocompatibility-complex-(MHC)-class-I-related molecule MR1 can present activating and non-activating vitamin-B-based ligands to mucosal-associated invariant T cells (MAIT cells). Whether MR1 binds other ligands is unknown. Here we identified a range of small organic molecules, drugs, drug metabolites and drug-like molecules, including salicylates and diclofenac, as MR1-binding ligands. Some of these ligands inhibited MAIT cells ex vivo and in vivo, while others, including diclofenac metabolites, were agonists...
February 6, 2017: Nature Immunology
Laurencas Raslavičius, Liudas Bazaras, Artūras Keršys, Vaidas Lukoševičius, Rolandas Makaras, Valdas Eidukynas
Bicycle riders are among the highest risk group in traffic. A cyclist simulation study captured kinematics and injuries to legs, pelvis, neck, and head for one human body size. We analyzed the number of parameters (forces acting on left and right tibia, head injury criterion, neck tensile force, neck shear force, and pelvic acceleration) for each of the four different cases: bicyclist ride out-residential driveway, motorist overtaking-undetected bicyclist, bicyclist left turn-same direction, and bicyclist right turn-opposite direction...
February 1, 2017: Proceedings of the Institution of Mechanical Engineers. Part H, Journal of Engineering in Medicine
Abdullatif K Althunyan, Magdy A Darwish, Moataza M Abdel Wahab
INTRODUCTION: Bicycling is one of the most enjoyable aerobic exercises recommended for the promotion of an individual's health. The Eastern Province of Saudi Arabia has seen a huge increase in the number of people who cycle. People have different goals for bicycling, but the injuries they sustain are common. Most of them relate to overuse, particularly of lower body joints. This study was conducted to determine the prevalence of knee problems and factors associated with knee pain in cyclists...
January 2017: Journal of Family & Community Medicine
M Zheng, L Z Li, Z A Jiang, L H Li, Y G Feng, X H Fu
Objective: To explore the different effects of chronic treatment with glibenclamide and gliclazide on the warm-up phenomenon in diabetes patients with coronary artery disease. Methods: A total of seventy-one patients with chronic stable angina and diabetes who were positive for exercise test and was proven that the stenosis degree was 70%-90% in at least one major branch through coronary angiogram were included into the study.They were divided into three groups, diet control group (DMD), glibenclamide group (DMG1) and gliclazide group (DMG2), according to the treatment of diabetes...
January 17, 2017: Zhonghua Yi Xue za Zhi [Chinese medical journal]
John R Rebula, Lauro V Ojeda, Peter G Adamczyk, Arthur D Kuo
Humans perform a variety of feedback adjustments to maintain balance during walking. These include lateral footfall placement, and center of pressure adjustment under the stance foot, to stabilize lateral balance. A less appreciated possibility would be to steer for balance like a bicycle, whose front wheel may be turned toward the direction of a lean to capture the center of mass. Humans could potentially combine steering with other strategies to distribute balance adjustments across multiple degrees of freedom...
December 1, 2016: Journal of Biomechanics
Courtney Coughenour, Alexander Paz, Hanns de la Fuente-Mella, Ashok Singh
No abstract text is available yet for this article.
December 2, 2016: Journal of Public Health
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