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https://www.readbyqxmd.com/read/28820600/magnesiate-addition-ring-expansion-strategy-to-access-the-6-7-6-tricyclic-core-of-hetisine-type-c20-diterpenoid-alkaloids
#1
Jason J Pflueger, Louis C Morrill, Justine N deGruyter, Melecio A Perea, Richmond Sarpong
A synthetic strategy to access the fused 6-7-6 tricyclic core of hetisine-type C20-diterpenoid alkaloids is reported. This strategy employs a Diels-Alder cycloaddition to assemble a fused bicyclic anhydride intermediate, which is elaborated to a vinyl lactone-acetal bearing an aromatic ring in five steps. Aromatic iodination is followed by magnesium-halogen exchange with a trialkyl magnesiate species, which undergoes intramolecular cyclization. Subsequent oxidation provides the desired 6-7-6 tricyclic diketoaldehyde, with carbonyl groups at all three positions for eventual C-N bond formation and subsequent elaboration...
August 18, 2017: Organic Letters
https://www.readbyqxmd.com/read/28820463/cycle-tracks-and-parking-environments-in-china-learning-from-college-students-at-peking-university
#2
Changzheng Yuan, Yangbo Sun, Jun Lv, Anne C Lusk
China has a historic system of wide cycle tracks, many of which are now encroached by cars, buses and bus stops. Even with these conditions, college students still bicycle. On campuses, students park their bikes on facilities ranging from kick-stand-plazas to caged sheds with racks, pumps and an attendant. In other countries, including Canada, some of the newer cycle tracks need to be wider to accommodate an increasing number of bicyclists. Other countries will also need to improve their bike parking, which includes garage-basement cages and two-tiered racks...
August 18, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28819610/a-rare-case-of-massive-rotator-cuff-tear-and-biceps-tendon-rupture-with-posterior-shoulder-dislocation-in-a-young-adult-surgical-decision-making-and-outcome
#3
En Loong Soon, Hamid Rahmatullah Bin Abd Razak, Andrew Hwee Chye Tan
INTRODUCTION: Massive rotator cuff tears (RCTs) in the context of shoulder dislocations are relatively uncommon in the young adult (<40 years) and if reported are more commonly described in association with acute traumatic anterior glenohumeral dislocations. They have rarely been described with posterior dislocations, regardless of patient age. This is the 1(st) case reported in the context of posterior dislocations, where a triad of biceps tendon rupture, posterior dislocation, and RCTs was observed during surgery...
March 2017: Journal of Orthopaedic Case Reports
https://www.readbyqxmd.com/read/28818462/discovery-of-non-zwitterionic-aryl-sulfonamides-as-nav1-7-inhibitors-with-efficacy-in-preclinical-behavioral-models-and-translational-measures-of-nociceptive-neuron-activation
#4
Yong-Jin Wu, Jason Guernon, Andrea McClure, Guanglin Luo, Ramkumar Rajamani, Alicia Ng, Amy Easton, Amy Newton, Clotilde Bourin, Dawn Parker, Kathleen Mosure, Omar Barnaby, Matthew G Soars, Ronald J Knox, Michele Matchett, Rick Pieschl, James Herrington, Ping Chen, D V Sivarao, Linda J Bristow, Nicholas A Meanwell, Joanne Bronson, Richard Olson, Lorin A Thompson, Carolyn Dzierba
Since zwitterionic benzenesulfonamide Nav1.7 inhibitors suffer from poor membrane permeability, we sought to eliminate this characteristic by replacing the basic moiety with non-basic bicyclic acetals and monocyclic ethers. These efforts led to the discovery of the non-zwitterionic aryl sulfonamide 49 as a selective Nav1.7 inhibitor with improved membrane permeability. Despite its moderate cellular activity, 49 exhibited robust efficacy in mouse models of neuropathic and inflammatory pain and modulated translational electromyogram measures associated with activation of nociceptive neurons...
August 9, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28813872/mit-skywalker-evaluating-comfort-of-bicycle-saddle-seat
#5
Rogerio S Goncalves, Taya Hamilton, Ali R Daher, Hiroaki Hirai, Hermano I Krebs
The MIT-Skywalker is a robotic device developed for the rehabilitation of gait and balance after a neurological injury. This device has been designed based on the concept of a passive walker and provides three distinct training modes: discrete movement, rhythmic movement, and balance training. In this paper, we present our efforts to evaluate the comfort of a bicycle/saddle seat design for the system's novel actuated body weight support device. We employed different bicycle and saddle seats and evaluated comfort using objective and subjective measures...
July 2017: IEEE ... International Conference on Rehabilitation Robotics: [proceedings]
https://www.readbyqxmd.com/read/28812886/room-temperature-ring-opening-of-quinoline-isoquinoline-and-pyridine-with-low-valent-titanium
#6
Seung-Yeol Baek, Takashi Kurogi, Dahye Kang, Masahiro Kamitani, Seongyeon Kwon, Douglas Solowey, Chun-Hsing Chen, Maren Pink, Patrick J Carroll, Daniel J Mindiola, Mu-Hyun Baik
The complex (PNP)Ti=CHtBu(CH2tBu) (PNP = N[2-PiPr2-4-methylphenyl]2-) dehydrogenates cyclohexane to cyclohexene by forming a transient low-valent titanium-alkyl species, [(PNP)Ti(CH2tBu)], which reacts with two equivalents of quinoline (Q) at room temperature to form H3CtBu and a Ti(IV) species where the less hindered C2=N1 bond of Q is ruptured and coupled to another equivalent of Q. The product isolated from this reaction is an imide with a tethered cycloamide group, (PNP)Ti=N[C18H13N] (1). Under photolytic conditions, intramolecular C-H bond activation across the imide-moiety in 1 occurs to form 2, and thermolysis reverses this process...
August 16, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28812404/effects-of-a-low-resistance-interval-bicycling-intervention-in-parkinson-s-disease
#7
Mehmet Uygur, Maria Bellumori, Christopher A Knight
Previous studies have shown that people with Parkinson's disease (PD) benefit from a variety of exercise modalities with respect to symptom management and function. Among the possible exercise modalities, speedwork has been identified as a promising strategy, with direct implications for the rate and amplitude of nervous system involvement. Considering that previous speed-based exercise for PD has often been equipment, personnel and/or facility dependent, and often time intensive, our purpose was to develop a population-specific exercise program that could be self-administered with equipment that is readily found in fitness centers or perhaps the home...
August 16, 2017: Physiotherapy Theory and Practice
https://www.readbyqxmd.com/read/28810083/self-cyclizing-antioxidants-to-prevent-dna-damage-caused-by-hydroxyl-radical
#8
Safnas F AbdulSalam, Purujit N Gurjar, Haizhou Zhu, Emma S Johnson, Jing Liu, Ana Luisa Kadekaro, Julio Landero-Figueroa, Edward Joseph Merino
Antioxidant therapy is a promising treatment strategy to protect DNA from damage caused by reactive oxygen species. Here we report novel self-cyclizing antioxidant reagents that are selective for hydroxyl radical. Our mechanistic investigation revealed that the reagents react with three equivalents of oxidant in a cascading reaction to form a bicyclic final product. Among the reagents synthesized 1c showed favourable properties in vitro and in cellular studies. Using As2O3, which triggers reactive oxygen species production, we showed 1c prevents formation of the guanine oxidation product 2,2,4-triamino-2H-oxazol-5-one-2'-deoxyribonucleoside and lowers levels of cellular reactive oxygen...
August 15, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28808202/-borneol-is-neuroprotective-against-permanent-cerebral-ischemia-in-rats-by-suppressing-production-of-proinflammatory-cytokines
#9
Lei Chang, Chun-Yu Yin, Hai-Yin Wu, Bin-Bin Tian, Yan Zhu, Chun-Xia Luo, Dong-Ya Zhu
Stroke is one of the leading causes of disability and death globally. It occurs when a major artery is occluded in the brain and leads to death of cells within the injured tissue. (+)-Borneol, a simple bicyclic monoterpene extracted from traditional Chinese medicine, is widely used in various types of diseases. However, no study has proved the effects of (+)-borneol on functional recovery from permanent ischemic stroke and the mechanism is still unknown. Here, we report that in the rat model of permanent cerebral ischemia, we found that (+)-borneol (1...
July 13, 2017: Journal of Biomedical Research
https://www.readbyqxmd.com/read/28803767/semantic-control-deficits-impair-understanding-of-thematic-relationships-more-than-object-identity
#10
Hannah Thompson, James Davey, Paul Hoffman, Glyn Hallam, Rebecca Kosinski, Sarah Howkins, Emma Wooffindin, Rebecca Gabbitas, Elizabeth Jefferies
Recent work has suggested a potential link between the neurocognitive mechanisms supporting the retrieval of events and thematic associations (i.e., knowledge about how concepts relate in a meaningful context) and semantic control processes that support the capacity to shape retrieval to suit the circumstances. Thematic associations and events are inherently flexible: the meaning of an item changes depending on the context (for example, lamp goes with reading, bicycle and police). Control processes might stabilise weak yet currently-relevant interpretations during event understanding...
August 10, 2017: Neuropsychologia
https://www.readbyqxmd.com/read/28800368/unpredictability-does-not-hamper-nonretinotopic-motion-perception
#11
Marc M Lauffs, Haluk Ögmen, Michael H Herzog
The motion of parts of an object is usually perceived relative to the object, i.e., nonretinotopically, rather than in retinal coordinates. For example, we perceive a reflector to rotate on the wheel of a moving bicycle even though its trajectory is cycloidal on the retina. The rotation is perceived because the motion of the object (bicycle) is discounted from the motion of its parts (reflector). It seems that the visual system can easily compute the object motion and subtract it from the part motion. Bikes move usually rather predictably...
August 1, 2017: Journal of Vision
https://www.readbyqxmd.com/read/28800241/diastereoselective-synthesis-of-diquinanes-and-triquinanes-bearing-vicinal-quaternary-carbon-stereocenters-from-acyclic-allene-based-precursors-via-a-cascade-reaction
#12
Shuang Li, Pengpeng Zhang, Yuanhe Li, Shumin Lu, Jianxian Gong, Zhen Yang
A cascade benzenethiol-mediated intramolecular [3 + 2] cycloaddition reaction between an allene and an α,β-unsaturated aldehyde or ester is developed for the diastereoselective synthesis of [3.3.0] bicyclic system bearing two quaternary atoms at their bridgehead positions. Notably, these structurally complex systems can be found in a wide range of natural products.
August 11, 2017: Organic Letters
https://www.readbyqxmd.com/read/28793052/cordyceps-sinensis-promotes-immune-regulation-and-enhances-bacteriostatic-activity-of-pa-824-via-il-10-in-mycobacterium-tuberculosis-disease
#13
D G Li, Z X Ren
PA-824 is a novel bicyclic nitroimidazole anti-tuberculosis (TB) drug. Cordyceps sinensis (Berk.) Sacc. (CS) was proven to be a good immunomodulatory compound. This research aimed to investigate the effect of CS on PA-824 in Mycobacterium tuberculosis (M.tb) infected mice (female CBA/J mice, 6 to 8 weeks of age and 20±2 g of weight). Mice were randomly assigned to 4 groups: PA-824, CS, PA-824+CS, and control. To verify the effect of PA-824 and CS on M.tb, after drug administration, mice lungs were harvested and bacterial colony formations were measured...
August 7, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28790513/the-jeremiah-metzger-lecture-cancer-in-the-twenty-first-century-an-inside-view-from-an-outsider
#14
Edward J Benz
Cancer is not a single disease. The term refers to literally hundreds of illnesses sharing common features: inappropriate proliferation of imperfectly differentiated cell types, invasion of nearby vital structures, and spread to distant sites (metastasis). Invasiveness and metastasis distinguish cancers from benign tumors such as fibroids and meningiomas. Yet, each type is distinct, possessed of defining morphologic, histologic, biochemical, and genomic features that have allowed oncologists to develop a nosology that guides diagnosis and therapy...
2017: Transactions of the American Clinical and Climatological Association
https://www.readbyqxmd.com/read/28789895/imidazo-1-2-%C3%AE-pyridines-possess-adenosine-a1-receptor-affinity-for-the-potential-treatment-of-cognition-in-neurological-disorders
#15
Roslyn Lefin, Mietha M van der Walt, Pieter J Milne, Gisella Terre'Blanche
Previous research has shown that bicyclic 6:5-fused heteroaromatic compounds with two N-atoms have variable degrees of adenosine A1 receptor antagonistic activity. Prompted by this imidazo[1,2-α]pyridine analogues were synthesized and evaluated for their adenosine A1 and A2A receptor affinity via radioligand binding studies and subjected to a GTP shift assay to determine its adenosine A1 receptor agonistic or antagonistic functionality. Imidazo[1,2-α]pyridine, the parent scaffold, was found devoid of affinity for the adenosine A1 and A2A receptors...
July 29, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28783355/iminosugar-c-nitromethyl-glycosides-and-divergent-synthesis-of-bicyclic-iminosugars
#16
Sure Siva Prasad, Soundararasu Senthilkumar, Akriti Srivastava, Sundarababu Baskaran
An efficient one-pot method for the stereoselective synthesis of novel iminosugar C-nitromethyl glycosides is described. This new class of iminosugar glycosides has versatile nitromethyl functionality whose utility was further demonstrated in the single-step synthesis of bicyclic iminosugars. Under reagent-free conditions, the N-allyl-C-nitromethyl glycosides resulted in intramolecular cyclization to iminosugar-oximes, whereas under SET oxidation, they furnished cyclopropane-fused iminosugars. The N-propargyl-C-nitromethyl glycosides underwent an unprecedented ketenimine-acrylamidine-Michael addition cascade reaction to give bicyclic amidines...
August 7, 2017: Organic Letters
https://www.readbyqxmd.com/read/28781179/injuries-and-illnesses-occurring-on-a-recreational-bicycle-tour-the-great-ohio-bicycle-adventure
#17
Thomas L Pommering, Diane C Manos, Bhavna Singichetti, Chelsea R Brown, Jingzhen Yang
OBJECTIVE: Recreational multiday cycling events have grown popular in the United States; however, little has been published regarding the injuries and illnesses that occur during these events. The objective of this study was to describe injuries and illnesses that occur in the Great Ohio Bicycle Adventure (GOBA) and to examine associated risk factors. METHODS: Injury and illness data collected from an on-site medical clinic during the 2013 and 2014 GOBA tours were merged with rider registration data for analysis...
August 3, 2017: Wilderness & Environmental Medicine
https://www.readbyqxmd.com/read/28780860/selective-catalytic-b-h-arylation-of-o-carboanyl-aldehydes-by-a-transient-directing-strategy
#18
Xiaolei Zhang, Hongning Zheng, Jie Li, Fei Xu, Jing Zhao, Hong Yan
Carboranyl aldehydes are among the most useful synthons in derivatization of carboranes. However, compared to the utilization of carboranyl carboxylic acids in selective B-H bond functionalizations, the synthetic application of carboranyl aldehydes is limited due to the weakly coordinating nature of aldehyde group. Herein, the direct arylation of o-carboranyl aldehydes has been developed via Pd-catalyzed cage B-H bond functionalization. With the help of glycine to generate a directing group (DG) in situ, a series of cage B(4,5)-diarylated- and B(4)-monoarylated-o-carboranyl aldehydes were obtained in good to excellent yields with high selectivity...
August 6, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28780534/applying-the-health-action-process-approach-to-bicycle-helmet-use-and-evaluating-a-social-marketing-campaign
#19
Florian M Karl, Jennifer Smith, Shannon Piedt, Kate Turcotte, Ian Pike
BACKGROUND: Bicycle injuries are of concern in Canada. Since helmet use was mandated in 1996 in the province of British Columbia, Canada, use has increased and head injuries have decreased. Despite the law, many cyclists do not wear a helmet. Health action process approach (HAPA) model explains intention and behaviour with self-efficacy, risk perception, outcome expectancies and planning constructs. The present study examines the impact of a social marketing campaign on HAPA constructs in the context of bicycle helmet use...
August 5, 2017: Injury Prevention: Journal of the International Society for Child and Adolescent Injury Prevention
https://www.readbyqxmd.com/read/28778011/dynamic-bicycle-exercise-to-assess-cardiac-output-at-multiple-exercise-levels-during-magnetic-resonance-imaging
#20
Johan Heiberg, Benjamin Asschenfeldt, Marie Maagaard, Steffen Ringgaard
PURPOSE: The aim was to establish a method for performing dynamic exercise during magnetic resonance imaging (MRI) using a slowly increasing workload protocol. METHODS: An ergometer bicycle with a step-wise, exercise protocol was used. Real-time phase-contrast MRI images of the aorta were obtained at each exercise step. RESULTS: In total, 40 participants completed the exercise protocol to reach a mean maximum cardiac output of 13.7±3.7l/min and a heart rate of 150±16beats/min at the highest exercise level...
July 27, 2017: Clinical Imaging
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