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Mukesh Kumar, Pankaj Chauhan, Arto Valkonen, Kari Rissanen, Dieter Enders
A highly stereoselective triple domino reaction for the synthesis of functionalized tricyclic chromane scaffolds has been developed. A secondary amine-catalyzed domino Michael/Michael/aldol condensation reaction between aliphatic aldehydes, nitro-chromenes, and α,β-unsaturated aldehydes leads to the formation of synthetically important tricyclic chromanes bearing four contiguous stereogenic centers including a tetrasubstituted carbon in good yields (20-66%) and excellent stereoselectivities (>20:1 dr and >99% ee)...
May 23, 2017: Organic Letters
Verónica Selva, Olatz Larrañaga, Luis M Castelló, Carmen Nájera, José M Sansano, Abel de Cozar
Diastereoselective multicomponent reaction of enantioenriched 4-nitroprolinates, obtained by enantiocatalyzed 1,3-dipolar cycloaddition (1,3-DC) of imino esters and nitroalkenes, with α,β-unsaturated aldehydes and electrophilic alkenes proceed with total periselectivity depending on the structure of the aldehyde employed. This process evolves through a [3+2] 1,3-DC when cinnamaldehyde is used in the presence of an azomethine ylide giving the corresponding highly substituted pyrrolizidines with endo-selectivity...
May 23, 2017: Journal of Organic Chemistry
Andrew O Kadlec, Dawid S Chabowski, Karima Ait-Aissa, Joseph C Hockenberry, Mary F Otterson, Matthew J Durand, Julie K Freed, Andreas M Beyer, David D Gutterman
Blood flow through healthy human vessels releases NO to produce vasodilation, whereas in patients with coronary artery disease (CAD), the mediator of dilation transitions to mitochondria-derived hydrogen peroxide (mtH2O2). Excessive mtH2O2 production contributes to a proatherosclerotic vascular milieu. Loss of PGC-1α (peroxisome proliferator-activated receptor γ coactivator 1α) is implicated in the pathogenesis of CAD. We hypothesized that PGC-1α suppresses mtH2O2 production to reestablish NO-mediated dilation in isolated vessels from patients with CAD...
May 22, 2017: Hypertension
Tim Oswald, Mira Diekmann, Annika Frey, Marc Schmidtmann, Rüdiger Beckhaus
The isotypic crystal structures of two titanocene complexes containing an EMe3 unit (E = Al, Ga; Me = meth-yl) with two μ2-coordinating methyl groups, namely [μ-1(η(5))-(adamantan-1-yl-2κC(1))cycylo-penta-dien-yl]di-μ2-methyl-methyl-2κC-[1(η(5))-penta-methyl-cyclo-penta-dien-yl]aluminiumtitanium(III), [AlTi(CH3)3(C10H15)(C15H18)], and [μ-1(η(5))-(adamantan-1-yl-2κC(1))cycylo-penta-dien-yl]di-μ2-methyl-methyl-2κC-[1(η(5))-penta-methyl-cyclo-penta-dien-yl]galliumtitanium(III), [GaTi(CH3)3(C10H15)(C15H18)], are reported...
May 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
Masaaki Ito, Shin-Ichiro Egashira, Kazuki Yoshida, Tomoko Mineno, Kazuo Kumagai, Hirotatsu Kojima, Takayoshi Okabe, Tetsuo Nagano, Michio Ui, Isao Matsuoka
AIMS: The P2Y6 nucleotide receptor is widely involved in inflammatory responses, and is a promising molecular target for the treatment of inflammatory diseases. Although several P2Y6 receptor antagonists have been developed and evaluated thus far, none has successfully been developed into a therapeutic drug. In this study, we explored new promising compounds that inhibit the human P2Y6 receptor. MAIN METHODS: High-throughput screening (HTS) was used to study the effects of various compounds on human P2Y6 receptors expressed in 1321N1 human astrocytoma cells by monitoring intracellular Ca(2+) concentration ([Ca(2+)]i) levels using an FDSS7000 real-time fluorescence detector...
May 17, 2017: Life Sciences
Sarah M Mosaad, Sawsan A Zaitone, Abdelazim Ibrahim, Amani A El-Baz, Dina M Abo-Elmatty, Yasser M Moustafa
The mechanism of celecoxib cardiovascular adverse events was earlier investigated; yet in-depth investigations are needed to assess the involvement of its pro-apoptotic effect throughout this process. An in-vivo chronic rat model of pressure overload employing Nʷ-nitro-l-arginine methyl ester (L-NAME) was tested at different time intervals to ensure the occurrence of persistent myocardial apoptosis along with pressure overload. Seven groups of male Wistar rats were assigned as (i) distilled water; (ii-iv) L-NAME (60 mg/kg) for 6, 12 or 16 weeks; (v-vii) L-NAME [16 weeks] + celecoxib (25, 50 or 100 mg/kg), from week 13 to week 16...
May 16, 2017: Chemico-biological Interactions
Jamshid Behin, Abbas Akbari, Mohsen Mahmoudi, Mehdi Khajeh
In present work, the treatment of aromatic compounds of simulated wastewater was performed by Fenton and NaOCl/Fe(2+) processes. The model solution was prepared based on the wastewater composition of Diisocyanate unit of Karoon Petrochemical Company/Iran containing Diamino-toluenes, Nitro-phenol, Mononitro-toluene, Nitro-cresol, and Dinitro-toluene. Experiments were conducted in a batch mode to examine the effects of operating variables such as pH, oxidant dosages, ferrous ion concentration and numbers of feeding on COD removal...
May 9, 2017: Water Research
Prasenjit Sau, Sourav Kumar Santra, Amitava Rakshit, Bhisma K Patel
A sequential construction of C-C, C-O, C=N and C=O bonds from alkenes leading to the direct synthesis of isoxazolines in the presence of tert-butyl nitrite, quinoline and Sc(OTf)3 catalyst in DCE at 80 oC has been accomplished. An unprecedented consecutive three CH functionalisations of two styrenes are involved during this isoxazoline synthesis. In this radical mediated reaction one half of the aryl alkene is converted into intermediate 2-nitro ketone which serve as a 1,3-dipolarophile and undergo cycloaddition with the other half of unreacted aromatic terminal alkene...
May 18, 2017: Journal of Organic Chemistry
Magdalena Kusek, Anna Tokarska, Marcin Siwiec, Anna Gadek-Michalska, Bernadeta Szewczyk, Grzegorz Hess, Krzysztof Tokarski
Corticotropin-releasing hormone (CRH)-synthesizing parvocellular neuroendocrine cells (PNCs) of the hypothalamic paraventricular nucleus (PVN) play a key role in the activation of the hypothalamic-pituitary-adrenocortical (HPA) axis. Several studies have demonstrated that synaptic inputs to these cells may undergo stress-related enhancement but, on the other hand, it has been reported that exposition to the same stressor for prolonged time periods may induce a progressive reduction in the response of the HPA axis to homotypic stressors...
2017: Frontiers in Cellular Neuroscience
Sangeeta Adhikari, Giridhar Madras
A facile, one-step combustion synthesis in solution is reported for preparing hetero-architectured NiO/Ni nanocomposites using different organic fuels. The prepared nanocomposites were physicochemically characterized for crystal structure, functional groups, and morphology. It was found that the content of Ni in the nanocomposite varied due to different combustion fuels. A photocatalytic (PC) investigation of these nanocomposites was performed using rhodamine 6G (RG) under UV light. A citric acid combusted NiO/Ni (N-CA) composite containing 20% Ni phase showed the highest photoactivity in comparison to pure NiO due to its large porous channels and high surface area (∼28 ± 2 m(2) g(-1))...
May 17, 2017: Physical Chemistry Chemical Physics: PCCP
Sharon C-A Chen, Shilpa Patel, Wieland Meyer, Belinda Chapman, Hong Yu, Karen Byth, Peter G Middleton, Helena Nevalainen, Tania C Sorrell
In vitro bacterial-fungal interaction studies in cystic fibrosis (CF) have mainly focused on interactions between bacteria and Candida. Here we investigated the effect of Pseudomonas aeruginosa on the growth of Scedosporium/Lomentospora spp. Standard suspensions of P. aeruginosa (16 non-mucoid and nine mucoid isolates) were dropped onto paper disks, placed on lawns of Lomentospora prolificans (formerly Scedosporium prolificans) strain WM 14.140 or Scedosporium aurantiacum strain WM 11.78 on solid agar. The median inhibitory activity (mIz) was calculated for each fungal-bacterial combination...
May 16, 2017: Mycopathologia
Kazuhiro Ishiguro, Osamu Watanabe, Masanao Nakamura, Takeshi Yamamura, Masanobu Matsushita, Hidemi Goto, Yoshiki Hirooka
4-Chloro-7-nitro-2,1,3-benzoxadiazole (NBD-Cl) functions as a hapten and fluoresces upon binding to proteins. Therefore, fluorescence visualization of hapten-proteins is a feature of the colitis induced by NBD-Cl. Using this colitis model, we located activated fibroblasts in the vicinity of hapten-proteins upon colitis induction and observed interleukin (IL)-6 production in the activated fibroblasts. We screened herbal ingredients using primary fibroblasts stimulated with tumor necrosis factor α (TNF-α) and found the suppressive action of Atractylodin on IL-6 production...
May 13, 2017: Clinical Immunology: the Official Journal of the Clinical Immunology Society
Jennifer A Ciezak-Jenkins, G M Borstad, I G Batyrev
The high-pressure behavior of 3,4-bis(4-nitro-1,2,5-oxadiazol-3-yl)-1,2,5-oxadiazole (LLM-172) has been studied to 36 GPa by Raman spectroscopy and 50 GPa by X-ray diffraction. The Raman spectra and calculated unit-cell volumes at select pressures show reasonable qualitative agreement with first-principles density functional theory calculations. Raman peaks exhibit a gradual broadening and loss of intensity upon compression to near 20 GPa. Above 20 GPa, most Raman features disappear with the exception of modes associated with the skeletal ring modes...
May 24, 2017: Journal of Physical Chemistry. A
Ning Lu, Ruxu Li, Zhonglin Wei, Jungang Cao, Dapeng Liang, Yingjie Lin, Haifeng Duan
No abstract text is available yet for this article.
May 16, 2017: Journal of Organic Chemistry
Firas H Kobeissy, Joy Guingab-Cagmat, Adriaan W Bruijnzeel, Mark S Gold, Kevin Wang
Second-hand smoke (SHS) exposure leads to the death of approximately 48,000 nonsmokers per year in the United States alone. SHS exposure has been associated with cardiovascular, respiratory, and neurodegenerative diseases. While cardiac function abnormalities and lung cancer due to SHS have been well characterized, brain injury due to SHS has not undergone a full systematic evaluation. Oxidative stress and nitration have been associated with smoking and SHS exposure. Animal studies suggest that exposure to tobacco smoke increases oxidative stress...
2017: Methods in Molecular Biology
Geetanjali Rampal, Tarunpreet Singh Thind, Rohit Arora, Adarsh Pal Vig, Saroj Arora
Although plant foods provide an array of nutrients in the human diet, our knowledge of how these nutrients are interacting among each other at molecular level is limited. Among these, glucosinolates are the most important secondary metabolites, which are readily hydrolyzed to a variety of products including isothiocyanates. The current study emphasizes on the antimutagenic potential of three isothiocyanates (ITCs) viz. allyl, benzyl and 3-butenyl ITCs (individually and in binary combinations) in Ames Salmonella histidine reversion assay using Salmonella typhimurium TA98 and TA100 tester strains...
May 12, 2017: Food and Chemical Toxicology
Qaiser Mahmood, Yanning Zeng, Xinxin Wang, Yang Sun, Wen-Hua Sun
A new family of nickel halides (bromides Ni1-Ni5 and chlorides Ni6-Ni10) ligated by 1-(2,6-dibenzhydryl-4-nitrophenylimino)-2-(arylimino)acenaphthylene (Aryl = 2,6-Me2C6H3L1, 2,6-Et2C6H3L2, 2,6-(i)Pr2C6H3L3, 2,4,6-Me3C6H2L4, and 2,6-Et2-4-MeC6H2L5) have been prepared and well characterized, and the scope of their catalytic properties toward the polymerization of ethylene has been investigated. Upon activation with either Et2AlCl or EASC, the nickel bromide complexes displayed better activities than their nickel chloride counterparts and produced higher-molecular-weight polyethylene in the range of 10(6) g mol(-1) with a very narrow range of molecular weight distributions...
May 15, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
Serhat Köseoğlu, Tuğba Pekbağr Yan K, Ebru Kucukyilmaz, Mehmet Sağlam, Sukru Enhos, Ayşe Akgün
This study evaluated four root repair materials for cytotoxicity and cell attachment in vitro. Cell viability was determined at 24 hr, 3 days and 7 days by using a 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide (XTT) assay with material extracts. Cell adhesion was examined with a scanning electron microscope on the surface of materials at 24 and 48 hr. Angelus MTA displayed the lowest cell viabilities at all-day incubations. Endocem had high biocompatibility on the first day. After culturing for 3 days and 7 days, the cell viabilities of Biodentine, Endocem and MM-MTA had similar results, and their cell viability was significantly higher than that of Angelus...
May 15, 2017: Microscopy Research and Technique
Jian Zhang, Liang Wang, Yi Shao, Yanqin Wang, Bruce Gates, Feng-Shou Xiao
This work delineates the persuasive example for controlling the steric adsorption of molecules on metal nanoparticles by zeolite crystals, thus enhancing the selectivity in hydrogenation of reactants with more than one reducible group. Key to this success is by fixing Pd nanoparticle inside of Beta zeolite crystals to form a fixed structure (Pd@Beta). In hydrogenation of substituted nitroarenes with multiple reducible groups as model reaction, the Pd@Beta exhibits superior selectivity for the hydrogenation of the nitro group, outperforming both conventional Pd nanoparticles supported on zeolite crystals and a commercial Pd/C catalyst...
May 14, 2017: Angewandte Chemie
Ke Wang, Xue Mao, Liling Cao, Guoping Lv, Xinfeng Dong, Yan He, Yongju Wei
Based on the photoinduced electron transfer (PET) principle, 4-amino-7-nitro-2,1,3-benzoxadiazole (ANBD) has been used as a fluorophore to develop a new fluorescent probe, 4-(2-N,N-dimethylthioacetamide)amino-7-nitro-2,1,3-benzoxadiazole (2), for the detection of Hg(2+). Upon the addition of Hg(2+), a 46-fold fluorescence enhancement occurs. Moreover the probe 2 exhibits a high selectivity and sensitivity to Hg(2+), even in the presence of other common metal ions. Under optimal reaction conditions, a good linearity can be obtained in the range of 0...
May 13, 2017: Journal of Fluorescence
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