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Samuel Aubert-Nicol, Jean Lessard, Claude Spino
A synthesis of the ABDE tetracyclic carbon core of palau'amine was achieved in 9 steps from commercial materials. The core's most notable feature, a highly strained trans cyclopenta[ c]pyrrolidine, was obtained in high yield using a ring contraction strategy starting from a much less strained trans bicyclic lactam derivative that is accessible in only 7 steps.
April 18, 2018: Organic Letters
Fei Wang, Mohammad Rafiee, Shannon S Stahl
An electrochemical protocol has been developed for α-oxygenation of cyclic carbamates by using a bicyclic aminoxyl as a mediator and water as the nucleophile. The mediated electrochemical method enables substrate oxygenation to proceed approximately 1 V lower than the redox potential of carbamate substrate. This feature allows for functional-group compatibility that is inaccessilble with conventional Shono oxidations that proceed via direct electrochemical substrate oxidation. This chemistry also represents the first α-functionalization of non-activated cyclic carbamates with oxoammonium as the oxidant...
April 16, 2018: Angewandte Chemie
Gagandeep Singh, Gurjit Singh, Rajbir Bhatti, Mehak Gupta, Ajay Kumar, Ankita Sharma, Mohan Paul Singh Ishar
A library of indolyl-isoxazolidines (6-9) has been synthesized by regio- and stereoselective microwave irradiated 1,3-dipolar cycloadditions of C-(3-indolyl)-N-phenylnitrone (2') with variedly substituted dipolarophiles (3'-5') and screened for their anti-inflammatory activities through inhibition of pro-inflammatory cytokines such as TNF-α and IL-6. Amongst the evaluated compounds (6-9), bicyclic isoxazolidine (9a) was found to exhibit significant inhibitory potential against LPS induced human IL-6 and TNF-α in THP-1 cells...
April 3, 2018: European Journal of Medicinal Chemistry
Kathryn Linkens, Hayden R Schmidt, James J Sahn, Andrew C Kruse, Stephen F Martin
Substituted norbenzomorphans are known to display high affinity and selectivity for the two sigma receptor (σR) subtypes. In order to study the effects of simplifying the structures of these compounds, a scaffold hopping strategy was used to design several novel sets of substituted isoindolines, tetrahydroisoquinolines and tetrahydro-2-benzazepines. The binding affinities of these new compounds for the sigma 1 (σ1R) and sigma 2 (σ2R) receptors were determined, and some analogs were identified that exhibit high affinity (Ki  ≤ 25 nM) and significant selectivity (>10-fold) for σ1R or σ2R...
March 29, 2018: European Journal of Medicinal Chemistry
Ju Cai, Bing Wu, Guangwei Rong, Cheng Zhang, Lihua Qiu, Xinfang Xu
An unprecedented gold-catalyzed bicyclization reaction of diaryl alkynes has been developed for the synthesis of indoles in good to high yields. Mechanistically, this alkyne bifunctionalization transformation was terminated by a stepwise formal X-H insertion reaction to furnish the corresponding polycyclic-frameworks with structural diversity, and the key intermediate 3 H-indole was isolated and characterized for the first time. In addition, further transformation of these generated tetracyclic-indoles with PCC as the oxidant provided straightforward access to the spirooxindoles in high yields...
April 13, 2018: Organic Letters
Gernot O Hering, Ewald M Hennig, Hartmut J Riehle, Jens Stepan
During a continuously increasing exercise workload (WL) a point will be reached at which arterial lactate accumulates rapidly. This so-called lactate threshold (LT) is associated with the maximal lactate steady state workload (MLSSW ), the highest WL, at which arterial lactate concentration [LA] does not change. However, the physiological range in which the LT and the MLSSW occur has not been demonstrated directly. We used minor WL variations in the MLSSW range to assess arterial lactate kinetics in 278 treadmill and 148 bicycle ergometer exercise tests...
2018: Frontiers in Physiology
Hamza M Alrabai, Martin G Gesheff, Ahmed I Hammouda, Janet D Conway
Voluntary elbow extension is essential for optimal upper limb positioning required for daily living activities, particularly above-shoulder maneuvers. The authors present a case of traumatic brachial plexus injury in which paralysis of the musculature selectively supplied by the posterior cord was based on magnetic resonance imaging and nerve conduction studies. An attempt at a radial nerve graft at another center was not effective. Ipsilateral hand function improved after multiple local tendon transfers were performed...
April 9, 2018: Journal of Hand Surgery
Jelle Van Cauwenberg, Ilse De Bourdeaudhuij, Peter Clarys, Bas de Geus, Benedicte Deforche
PURPOSE: Electric bicycles (e-bikes) may offer an opportunity to stimulate physical activity among older adults. The current study compared Flemish (Belgian) older e-bike users against those not using an e-bike on socio-demographics, health characteristics and access to motorized transport. Additionally, it examined the association between e-bike use and levels of cycling and the moderating effects of sex, BMI and cycling limitations. METHODS: An online- or interview-version of the same questionnaire were completed by 1146 participants...
April 11, 2018: Medicine and Science in Sports and Exercise
Dafni Charisopoulou, George Koulaouzidis, Annika Rydberg, Michael Y Henein
BACKGROUND: Long QT syndrome (LQTS) carriers are characterized by abnormal ventricular repolarization, prolonged systole, and mechanical dispersion. Prolonged left ventricular (LV) systole has been shown to result in disproportionate shortening of LV filling in other conditions. The aim of this study was to assess LV filling, diastolic function, and stroke volume (SV) response to dynamic exercise, in a group of LQTS carriers. METHODS: Forty-seven LQTS carriers (45 ± 15 years, 20 symptomatic) and 35 healthy individuals underwent bicycle stress echocardiogram...
April 12, 2018: Echocardiography
Gergana Todorova Taneva Zaryanova, Ana Begoña Arribas Díaz, Ciro Baeza Bermejillo, César Aparicio Martínez, Alejandro González García
Complete transection of the common femoral artery is more frequent after penetrating injuries than after blunt trauma, with most of the cases occurring in combination with fractures. Contusion from a bicycle handlebar is a rare form of injury to the femoral vessels. Hereby, we present a case of complete common femoral artery transection caused by a direct bicycle handlebar trauma. The patient suffered severe hypovolemia during his transfer to the Emergency room. He required an emergency intervention and a bypass reconstruction...
June 2017: Trauma Case Reports
K P Debbink, D B Tashjian, M V Tirabassi, R Gaffey, J Nahmias
Ureteric trauma is rare, occurring in < 1% of all traumas. We present a unique case of a 13 year old female who sustained a penetrating abdominal injury from a bicycle handlebar. Upon initial examination there was herniation of bowel through the abdominal wound, so exploratory laparotomy was performed. A serosal injury of the colon and bleeding mesenteric veins were encountered; the retroperitoneum was not explored at that time. Postoperative course was remarkable for a doubling of the serum creatinine, increasing abdominal distention and pain...
August 2017: Trauma Case Reports
Jelle Hofman, Roeland Samson, Steven Joosen, Ronny Blust, Silvia Lenaerts
Urban environments typically exhibit large atmospheric pollution variation, in both space and time. In contrast to traditional monitoring networks suffering from a limited spatial coverage, mobile platforms enable personalized high-resolution monitoring, providing valuable insights into personal atmospheric pollution exposure, and the identification of potential pollution hotspots. This study evaluated personal cyclist exposure to UFPs, BC and heavy metals whilst commuting near Antwerp, Belgium, by performing mobile measurements with wearable black carbon (BC) and ultrafine particle (UFP) instruments...
April 4, 2018: Environmental Research
Marc M Lauffs, Oh-Hyeon Choung, Haluk Öğmen, Michael H Herzog
Unconscious visual stimuli can affect conscious perception: For example, an invisible prime can affect responses to a subsequent target. The invisible interpretation of an ambiguous figure can have similar effects. Invisibility in these situations is typically explained by stimulus-suppression in early, retinotopic brain areas. We have previously argued that invisibility is closely linked to Gestalt ("object") organization principles. For example, motion is typically perceived in non-retinotopic, object-centered, and not in retinotopic coordinates...
April 4, 2018: Consciousness and Cognition
Cheryl Kerfeld, Tracy Jirikowic, Katheryn J Allyn, Murray E Maitland
BACKGROUND: Through play, children develop motor, cognitive, social, and other life skills. Play barriers can impede physical and psychosocial benefits. OBJECTIVES: We describe participation in active play, fundamental movement skills, play environment characteristics, and potential play barriers for school-aged children (6-12 years) who use lower extremity prostheses. STUDY DESIGN: Cross-sectional questionnaire study. METHODS: A questionnaire was developed and administered online to parents of children 6-12 years who use lower extremity prostheses...
April 1, 2018: Prosthetics and Orthotics International
Micah G Katz, Stephen J Fenton, Kathryn W Russell, Eric R Scaife, Scott S Short
PURPOSE: To examine surgical outcomes of children with pancreaticoduodenal injuries at a Quaternary Level I pediatric trauma center. METHODS: We queried a prospectively maintained trauma database of a level one pediatric trauma center for all cases of pancreatic and/or duodenal injury from 2002 to 2017. Analysis was conducted using JMP 13.1.0. RESULTS: 170 children presented with pancreatic and/or duodenal injury. 13 (7.7%) suffered a combined injury and this group forms the basis for this report with mean ISS of 22...
April 5, 2018: Pediatric Surgery International
D G Fitzpatrick, M Goh, D C Howlett, M Williams
Cycling is a popular activity. However there are risks associated with cycling, including facial injury. Helmets are often worn to prevent head injury. Evidence for their protection against facial injury is limited. This meta-analysis investigated the effect of bicycle helmets on the incidence of facial injury. The PubMed/MEDLINE, Google Scholar, and Cochrane Library databases were searched. Studies included were observational and involved adult participants. Paediatric studies, studies on helmet legislation, and those combining facial injuries with other injury types were excluded...
April 2, 2018: International Journal of Oral and Maxillofacial Surgery
Mirao Zha, Ping Lin, Hongwei Yao, Yibing Zhao, Chuanliu Wu
Bicyclic peptides have been attractive scaffolds for developing high affinity reagents for biomacromolecules. Here we report a general phage-screening strategy for the development of bicyclic peptide ligands constrained with isomerically-forbidden disulfide bridges without elaborate chemical modifications and recourses to genetic code reprogramming.
April 5, 2018: Chemical Communications: Chem Comm
Mahesh Narain Tripathi, Sony Kumari, Tikhe Sham Ganpat
College students are vulnerable to a critical period in developmental maturation, facing rigorous academic work, and learning how to function independently. Physical activities such as running and bicycling have been shown to improve mood and relieve stress. However, college students often have low levels of physical activity. Yoga is an ancient physical and mental activity that affects mood and stress. However, studies examining the psychophysiological effects of yoga are rare in peer-reviewed journals. The aim of this study is to establish preliminary evidence for the psychophysiological effects of yoga on stress in young-adult college students...
2018: Journal of Education and Health Promotion
V Athanasiou, A Panagopoulos, I D Iliopoulos, I Vrahnis, G Diamantakis, P Kraniotis, M Tyllianakis
Background: Intra-articular fractures of the distal part of the triquetrum within the pisotriquetral joint are uncommon, and can be associated with tears of the dorsal carpal ligaments, pisiform subluxation and/or FCU dislocation. Their diagnosis is difficult and requires a high clinical suspicion and a proper radiological examination including oblique wrist x-rays, computed tomography and MRI scan. These fractures can be delayed diagnosed due to late presentation thus leading to painful nonunion, persistent instability and late pisotriquetral arthritis...
2018: Open Orthopaedics Journal
Xiaoxi Zhou, Fanping Huang, Chun Tang, Qingde Zhuo, Zhixin Chen, Hong Zhang, Haiping Xia
Despite the excellent chemical properties of N-heterocycles, pyrido[1,2-α]azepine remains elusive due to its potential antiaromaticity and lability. Herein, we demonstrate the synthesis and characterization of the first bicyclic pyrido[1,2-α]azepine that leverages the coordination to the ruthenium center to promote the stability of N-bridged bicycle.
April 4, 2018: Chemical Communications: Chem Comm
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