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https://www.readbyqxmd.com/read/28546832/phosphazene-catalyzed-desymmetrization-of-cyclohexadienones-by-dithiane-addition
#1
Matthew A Horwitz, Elisabetta Massolo, Jeffrey S Johnson
We report a desymmetrization of cyclohexadienones by intramolecular conjugate addition of a tethered dithiane nucleophile. Mild reaction conditions allow the formation of diversely functionalized fused bicyclic lactones. The products participate in facially selective additions from the convex surface, leading to allylic alcohol derivatives.
2017: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28544162/benzimidazole-scaffold-as-anticancer-agent-synthetic-approaches-and-structure-activity-relationship
#2
REVIEW
Neelima Shrivastava, Mohd Javed Naim, Md Jahangir Alam, Farah Nawaz, Shujauddin Ahmed, Ozair Alam
Cancer, also known as malignant neoplasm, is a dreadful disease which involves abnormal cell growth having the potential to invade or spread to other parts of the body. Benzimidazole is an organic compound that is heterocyclic and aromatic in nature. It is a bicyclic compound formed by the fusion of the benzene and imidazole ring systems. It is an important pharmacophore and a privileged structure in medicinal chemistry. According to the World Health Organisation (2015 survey), one in six deaths is due to cancer around the globe, accounting for 8...
May 22, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28541687/bicyclic-alkyl-amino-carbenes-bicaacs-stable-carbenes-more-ambiphilic-than-caacs
#3
Eder Tomás-Mendivil, Max M Hansmann, Cory M Weinstein, Rodolphe Jazzar, Mohand Melaimi, Guy Bertrand
A straightforward strategy allows for the synthesis of storable bicyclic (alkyl)(amino)carbenes (BICAACs), which feature enhanced σ-donating and π-accepting properties compared to monocyclic (alkyl)(amino)carbenes (CAACs). Due to the bicyclo[2.2.2]octane skeleton, the steric environment around the carbene center is different from that of CAACs, and similar to that observed in classical NHCs. The different electronic properties of BICAACs as compared to CAACs allow for ligand exchange reactions not only at a metal center, but also at main group elements...
May 25, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28541349/synthesis-of-spiro-quasi-1-catenanes-and-quasi-1-rotaxanes-via-a-templated-backfolding-strategy
#4
Luuk Steemers, Martin J Wanner, Martin Lutz, Henk Hiemstra, Jan H van Maarseveen
Due to their well-defined three-dimensional geometry, spiro compounds are widely utilized in drug research. From the central tetrahedral carbon atom, besides the regular structure, an inverted spiro connectivity may be envisioned. Here we disclose the synthesis of this molecule class that we have coined quasi[1]catenanes. Next to their fascinating and aesthetic shape, the higher compactness as compared to regular spiro bicycles is noteworthy. To enable synthetic access to compact entangled multimacrocyclic molecules, we have developed a new strategy...
May 25, 2017: Nature Communications
https://www.readbyqxmd.com/read/28540372/bis-and-mono-m-benzoic-acid-functionalized-pillar-5-arenes
#5
Xin-Lang Wu, Yi Chen, Wen-Jing Hu, Yahu A Liu, Xue-Shun Jia, Jiu-Sheng Li, Biao Jiang, Ke Wen
Installation of m-benzoic acid functionalities on pillar[5]arene rims resulted in bis- and mono(m-benzoic acid)-functionalized pillar[5]arenes 1 and 2. Bis(m-benzoic acid)-functionalized pillar[5]arene 1 was able to self-assemble to form one-dimensional channels with DMF molecules residing in pillar[5]arene cavities. Esterification of two carboxylic acids in 1 with decane-1,10-diol did not afford a [1]catenane, but a bicyclic compound. Although 1-decanol esterification of mono(m-benzoic acid)-functionalized pillar[5]arene 2 did not form a self-included [1]pseudorotaxane-like structure, a mono(decyl m-benzoate)-functionalized pillar[5]arene bearing an ethyl acetate chain was found to form a self-included complex with the ethyl acetate moiety residing inside the pillar[5]arene cavity...
May 25, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28539755/practical-synthesis-of-the-bicyclic-darunavir-side-chain-3r-3as-6ar-hexahydrofuro-2-3-b-furan-3-ol-from-monopotassium-isocitrate
#6
REVIEW
Gary L Moore, Rodger W Stringham, David S Teager, Tai-Yuen Yue
A practical synthesis of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-ol-a key intermediate in the synthesis of darunavir-from monopotassium isocitrate is described. The isocitric acid salt, obtained from a high-yielding fermentation fed by sunflower oil, was converted in several steps to a tertiary amide. This amide, along with the compound's ester functionalities, was reduced with lithium aluminum hydride to give, on acidic workup, a transient aminal-triol. This was converted in situ to the title compound, the bicyclic acetal furofuranol side chain of darunavir, a protease inhibitor used in treatment of HIV/AIDS...
January 20, 2017: Organic Process Research & Development
https://www.readbyqxmd.com/read/28539128/impaired-cardiac-output-during-exercise-in-adults-operated-for-ventricular-septal-defect-in-childhood-a-hitherto-unrecognised-pathophysiological-response
#7
Benjamin Asschenfeldt, Johan Heiberg, Steffen Ringgaard, Marie Maagaard, Andrew Redington, Vibeke E Hjortdal
BACKGROUND: Recent studies have demonstrated that surgical ventricular septal defect closure in childhood is associated with reduced functional capacity and disruption of the right ventricular force-frequency relationship during exercise. To further describe long-term cardiac function, we performed a non-invasive assessment of cardiac index during exercise in adults having undergone surgery for ventricular septal defect in early childhood. METHODS: A total of 20 patients (surgical age 2...
May 25, 2017: Cardiology in the Young
https://www.readbyqxmd.com/read/28537540/-e-bikers-are-more-often-seriously-injured-in-bicycle-accidents-results-from-the-groningen-bicycle-accident-database
#8
H P A M Poos, T L Lefarth, J S Harbers, K W Wendt, M El Moumni, I H F Reininga
OBJECTIVE: Analysing injury types, injury severity and mortality in victims of accidents with electric bicycles in comparison with conventional bicycles. DESIGN: Prospective cohort study. METHOD: Data of patients treated at the Accident & Emergency Department of the University Medical Center Groningen after a bicycle accident are being entered in a database since 2014. We have analysed this database for accidents with electric bicycles (e-bikes) and conventional bicycles occurring among adult patients for the period of July 2014 to May 2016...
2017: Nederlands Tijdschrift Voor Geneeskunde
https://www.readbyqxmd.com/read/28536145/monoterpenes-support-systemic-acquired-resistance-within-and-between-plants
#9
Marlies Riedlmeier, Andrea Ghirardo, Marion Wenig, Claudia Knappe, Kerstin Koch, Elisabeth Georgii, Sanjukta Dey, Jane E Parker, Joerg-Peter Schnitzler, Corina Vlot
This study investigates the role of volatile organic compounds in systemic acquired resistance (SAR), a salicylic acid (SA)-associated, broad-spectrum immune response in systemic, healthy tissues of locally infected plants. Gas chromatography coupled to mass spectrometry analyses of SAR-related emissions of wild-type and non-SAR-signal-producing mutant plants associated SAR with monoterpene emissions. Headspace exposure of Arabidopsis thaliana to a mixture of the bicyclic monoterpenes α-pinene and β-pinene induced defense, accumulation of reactive oxygen species, and expression of SA- and SAR-related genes, including the SAR regulatory AZELAIC ACID INDUCED1 (AZI1) gene and three of its paralogs...
May 23, 2017: Plant Cell
https://www.readbyqxmd.com/read/28535722/anisotropic-polyethersulfone-foam-for-bicycle-helmet-liners-to-reduce-rotational-acceleration-during-oblique-impact
#10
Kelly Vanden Bosche, Yasmine Mosleh, Bart Depreitere, Jos Vander Sloten, Ignaas Verpoest, Jan Ivens
Although current standard bicycle helmets protect cyclists against linear acceleration, they still lack sufficient protection against rotational acceleration during oblique impact events. Rotational acceleration is correlated with serious traumatic brain injuries such as acute subdural haematoma and thus should be minimized. This study proposes using highly anisotropic polyethersulfone foam for bicycle helmet liners in order to limit the rotational acceleration. Helmet prototypes, made of polyethersulfone foam with cell anisotropy direction perpendicular to the head, have been produced and compared to a standard commercial helmet...
May 1, 2017: Proceedings of the Institution of Mechanical Engineers. Part H, Journal of Engineering in Medicine
https://www.readbyqxmd.com/read/28535477/the-effect-of-crash-characteristics-on-cyclist-injuries-an-analysis-of-virginia-automobile-bicycle-crash-data
#11
Erin Robartes, T Donna Chen
This paper examines bicyclist, automobile driver, vehicle, environmental, and roadway characteristics that influence cyclist injury severity in order to determine which factors should be addressed to mitigate the worst bicyclist injuries. An ordered probit model is used to examine single bicycle-single vehicle crashes from Virginia police crash report data from 2010 to 2014. Five injury severity levels are considered: fatalities, severe injuries, minor or possible injuries, no apparent injuries, and no injury...
May 20, 2017: Accident; Analysis and Prevention
https://www.readbyqxmd.com/read/28534594/bicyclo-2-2-2-octane-1-4-dicarboxylic-acid-towards-transparent-metal-organic-frameworks
#12
P J Llabres-Campaner, J Pitarch-Jarque, R Ballesteros-Garrido, B Abarca, R Ballesteros, E García-España
The preparation of transparent porous materials can offer a different access towards the study of molecules under solid confined space. Metal-organic frameworks represent a unique opportunity due to their tunable pore size, however aromatic linkers present strong absorption and reduce the transparency. Herein, we report the first example of a MOF with bicyclic organic dicarboxylic linkers and its use as a solid solvent.
May 23, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28534004/integrating-health-and-transportation-in-nashville-tennessee-usa-from-policy-to-projects
#13
Leslie A Meehan, Geoffrey P Whitfield
The Nashville Area Metropolitan Planning Organization (MPO) is among the first MPOs in the United States to recognize the interplay of transportation and public health, particularly regarding physical activity, air pollution, and traffic crashes. The Nashville MPO has taken a multifaceted approach to simultaneously improve the transportation system, quality of life, and health status of the region's population. The purpose of this paper is to describe the multiple programs and projects that the MPO has undertaken to this end, so that other cities might learn from Nashville's example...
March 2017: Journal of Transport & Health
https://www.readbyqxmd.com/read/28530098/formal-total-synthesis-of-%C3%A2-lycojaponicumin-c
#14
Nan Zheng, Lijie Zhang, Jianxian Gong, Zhen Yang
The formal total synthesis of (±)-lycojaponicumin C has been accomplished. Key transformations include a Rh-catalyzed formal [3 + 2] cycloaddition reaction to construct the bicyclic [3.3.0] scaffold bearing two vicinal quaternary carbon centers, a stereoselective γ-hydroxyl directed Michael addition to introduce the vinyl group at a bulky position, and a late-stage ring-closing metathesis reaction to form the cyclohexanone ring.
May 22, 2017: Organic Letters
https://www.readbyqxmd.com/read/28524111/synthesis-and-pharmacological-properties-of-novel-esters-based-on-monoterpenoids-and-glycine
#15
Mariia Nesterkina, Iryna Kravchenko
Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via Steglich esterification and characterized by ¹H-NMR, IR, and mass spectral studies. Their analgesic and anti-inflammatory activities were investigated after transdermal delivery on models of formalin, capsaicin, and AITC-induced pain, respectively. Glycine esters of menthol and borneol exhibited higher antinociceptive action, whereas eugenol derivative significantly suppressed the development of the inflammatory process. The mechanism of competitive binding between terpenoid esters and TRPA1/TRPV1 agonists was proposed explaining significant analgesic effect of synthesized derivatives...
May 18, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28524077/highly-stereoselective-synthesis-of-a-compound-collection-based-on-the-bicyclic-scaffolds-of-natural-products
#16
Murali Annamalai, Stanimira Hristeva, Martyna Bielska, Raquel Ortega, Kamal Kumar
Despite the great contribution of natural products in the history of successful drug discovery, there are significant limitations that persuade the pharmaceutical industry to evade natural products in drug discovery research. The extreme scarcity as well as structural complexity of natural products renders their practical synthetic access and further modifications extremely challenging. Although other alternative technologies, particularly combinatorial chemistry, were embraced by the pharmaceutical industry to get quick access to a large number of small molecules with simple frameworks that often lack three-dimensional complexity, hardly any success was achieved in the discovery of lead molecules...
May 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28515841/demands-of-simulated-commuting-using-an-electrically-assisted-bicycle
#17
D Taylor LA Salle, Robert Shute, Matthew Heesch, Dustin Slivka
The American College of Sports Medicine (ACSM) recommends adults participate in weekly aerobic activity for a minimum of 30 minutes moderate intensity exercise 5 days per week or 20 minutes of vigorous activity 3 days per week. The electrically assisted bicycle may help individuals achieve the ACSM's aerobic recommendations and introduce inactive individuals to physical activity. To compare the physiological requirements of riding a bicycle with electric pedal assist versus non-assist among healthy active young adults...
2017: International Journal of Exercise Science
https://www.readbyqxmd.com/read/28514398/-structural-features-of-the-lipid-bilayer-of-the-red-blood-cell-membrane-in-people-with-isolated-hypercholesterolemia-without-coronary-artery-disease-and-in-patients-with-coronary-artery-disease
#18
A P Vasilev, N N Streltsova, N L Lystsova
AIM: To identify the specific features of modifying the lipid composition of the red blood cell membrane in people with isolated hypercholesterolemia without coronary heart disease (CHD) and in CHD patients with different functional classes of angina pectoris. SUBJECTS AND METHODS: 92 men with Functional Class II-IV stable angina, 22 men with isolated hypercholesterolemia (HC) without CHD, and 18 healthy men with normal cholesterol levels were examined. Blood plasma cholesterol levels were determined in all the examinees...
2017: Terapevticheskiĭ Arkhiv
https://www.readbyqxmd.com/read/28513291/low-cost-mobile-air-pollution-monitoring-in-urban-environments-a-pilot-study-in-lubbock-texas
#19
Grant R McKercher, Jennifer K Vanos
The complex nature of air pollution in urban areas due to meteorological influences and mobile emissions prevents traditional monitoring techniques from obtaining measurements representative of true human exposure. Small, mobile air pollution monitors, however, are useful tools to address this complexity. The current study assessed the capability of low-cost mobile monitors to acquire useful data in a city without a monitoring network in place (Lubbock, Texas) using a bicycle platform. The monitoring campaign resulted in 30 days of data along a 13...
May 17, 2017: Environmental Technology
https://www.readbyqxmd.com/read/28508899/the-quasi-unchanged-gas-phase-molecular-structures-of-the-atmospheric-aerosol-precursor-%C3%AE-pinene-and-its-oxidation-product-nopinone
#20
E M Neeman, J-R Avilés-Moreno, T R Huet
The rotational spectra of the two bicyclic molecules β-pinene and its oxidation product nopinone were investigated in the gas phase, using Fourier transform microwave spectroscopy coupled to a supersonic jet, in the 2-20 GHz range. The parent species and all heavy atom isotopologues have been observed in their natural abundance. The spectroscopic parameters of the ground states were determined from a Watson's Hamiltonian in the A reduction. The rotational constants were used together with geometrical parameters obtained from ab initio calculations to determine the r0 and r structures of the skeletons, without any structural assumption in the fit concerning the heavy atoms...
May 16, 2017: Physical Chemistry Chemical Physics: PCCP
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