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https://www.readbyqxmd.com/read/28203273/synthesis-and-biological-evaluation-of-the-new-1-3-dimethylxanthine-derivatives-with-thiazolidine-4-one-scaffold
#1
Sandra Constantin, Florentina Geanina Lupascu, Maria Apotrosoaei, Ioana Mirela Vasincu, Dan Lupascu, Frederic Buron, Sylvain Routier, Lenuta Profire
BACKGROUND: The xanthine structure has proved to be an important scaffold in the process of developing a wide variety of biologically active molecules such as bronchodilator, hypoglycemiant, anticancer and anti-inflammatory agents. It is known that hyperglycemia generates reactive oxygen species which are involved in the progression of diabetes mellitus and its complications. Therefore, the development of new compounds with antioxidant activity could be an important therapeutic strategy against this metabolic syndrome...
2017: Chemistry Central Journal
https://www.readbyqxmd.com/read/28198903/a-stereoselective-synthesis-of-e-or-z-%C3%AE-arylvinyl-halides-via-a-borylative-coupling-halodeborylation-protocol
#2
Jakub Szyling, Adrian Franczyk, Piotr Pawluć, Bogdan Marciniec, Jędrzej Walkowiak
A new stereoselective method for the synthesis of (E)-β-arylvinyl iodides and (E)- or (Z)-β-arylvinyl bromides from styrenes and vinyl boronates on the basis of a one-pot procedure via borylative coupling/halodeborylation is reported. Depending on the halogenating agent as well as the mode of the halodeborylation reaction, (E) or (Z) isomers are selectively formed.
February 15, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28198170/antibacterial-effect-of-sevoflurane-and-isoflurane
#3
M Martínez-Serrano, M Gerónimo-Pardo, A Martínez-Monsalve, M D Crespo-Sánchez
OBJECTIVE: Multidrug resistant bacteria are increasing worldwide and therapeutic options are limited. Some anaesthetics have shown antibacterial activity before. In this study, we have investigated the antibacterial effect of the halogenated anaesthetic agents sevoflurane and isoflurane against a range of resistant pathogens. METHODS: Two experiments were conducted. In the first, bacterial suspensions of both ATCC and resistant strains of Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were exposed to liquid sevoflurane and isoflurane during 15, 30 and 60 minutes...
February 15, 2017: Revista Española de Quimioterapia: Publicación Oficial de la Sociedad Española de Quimioterapia
https://www.readbyqxmd.com/read/28177237/direct-c-h-cyanation-of-arenes-via-organic-photoredox-catalysis
#4
Joshua B McManus, David A Nicewicz
Methods for the direct C-H functionalization of aromatic compounds are in demand for a variety of applications, including the synthesis of agrochemicals, pharmaceuticals, and materials. Herein, we disclose the construction of aromatic nitriles via direct C-H functionalization using an acridinium photoredox catalyst and trimethylsilyl cyanide under an aerobic atmosphere. The reaction proceeds at room temperature under mild conditions and has proven to be compatible with a variety of electron-donating and -withdrawing groups, halogens, and nitrogen- and oxygen-containing heterocycles, as well as aromatic-containing pharmaceutical agents...
February 14, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28161088/synthesis-and-qsar-study-of-novel-%C3%AE-methylene-%C3%AE-butyrolactone-derivatives-as-antifungal-agents
#5
Yong-Ling Wu, De-Long Wang, En-Hui Guo, Shuang Song, Jun-Tao Feng, Xing Zhang
Thirty-six new α-benzylidene-γ-lactone compounds based α-methylene-γ-butyrolactone substructure were prepared and characterized by spectroscopic analysis. All compounds were evaluated for antifungal activities in vitro against six plant pathogenic fungi and the half maximal inhibitory concentration (IC50) against Botrytis cinerea and Colletotrichum lagenarium were investigated. Compounds 5c-3 and 5c-5 with the halogen atom exhibited excellent fungicidal activity against B. cinerea (IC50=22.91, 18.89μM)...
January 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28133390/influence-of-antimony-halogen-additives-on-flame-propagation
#6
Valeri I Babushok, Peter Deglmann, Roland Krämer, Gregory T Linteris
A kinetic model for flame inhibition by antimony-halogen compounds in hydrocarbon flames is developed. Thermodynamic data for the relevant species are assembled from the literature, and calculations are performed for a large set of additional species of Sb-Br-C-H-O system. The main Sb- and Br-containing species in the combustion products and reaction zone are determined using flame equilibrium calculations with a set of possible Sb-Br-C-H-O species, and these are used to develop the species and reactions in a detailed kinetic model for antimony flame inhibition...
2017: Combust Sci Technol
https://www.readbyqxmd.com/read/28053569/synthesis-of-n-mannich-bases-of-berberine-linking-piperazine-moieties-revealing-anticancer-and-antioxidant-effects
#7
Bhupendra Mistry, Rahul V Patel, Young-Soo Keum, Doo Hwan Kim
A new Mannich base series of piperazine linked berberine analogues was furnished in this study to screen the antioxidant and anticancer potential of the resultant analogues. Alkoxy group at a C-9 position of berberine was converted to hydroxyl functionality to enhance the ability of final scaffolds binding to the target of drug action mainly through hydrophobic effect, conjugation effect, whereas Mannich base functionality was introduced on the C-12 position of berberine. Scaffolds were investigated for their free radical scavenging antioxidant potential in FRAP and DPPH assay, whereas tested to check their Fe(+3) reducing power in ABTS assay...
January 2017: Saudi Journal of Biological Sciences
https://www.readbyqxmd.com/read/28049918/trialkylamine-derivatives-containing-a-triazole-moiety-as-promising-ergosterol-biosynthesis-inhibitor-design-synthesis-and-antifungal-activity
#8
Guoqing Sui, Wen Zhang, Kun Zhou, Yulin Li, Bingyu Zhang, Dan Xu, Yong Zou, Wenming Zhou
As a part of our continuing research on amine derivative antifungal agents, 19 novel target compounds containing 1,2,4-triazole and tertiary amine moieties were designed and synthesized, and their in vitro antifungal activities against six phytopathogenic fungi (Magnaporthe grisea, Alternaria solani, Fusarium solani, Curvularia lunata, A. alternata, F. graminearum) were assayed. All target compounds were elucidated by means of (1)H-NMR, (13)C-NMR, high resolution (HR)-MS, and IR analysis. The results showed that most of the derivatives exhibited obvious activity against each of the fungi at 50 µg/mL...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28035962/literature-survey-and-further-studies-on-the-3-alkylation-of-n-unprotected-3-monosubstituted-oxindoles-practical-synthesis-of-n-unprotected-3-3-disubstituted-oxindoles-and-subsequent-transformations-on-the-aromatic-ring
#9
Eszter Kókai, Gyula Simig, Balázs Volk
The paper provides a comprehensive review of the base-catalysed C3-alkylation of N-unprotected-3-monosubstituted oxindoles. Based on a few, non-systematic studies described in the literature using butyllithium as the deprotonating agent, an optimized method has now been elaborated, via the corresponding lithium salt, for the selective C3-alkylation of this family of compounds. The optimal excess of butyllithium and alkylating agent, and the role of the halogen atom in the latter (alkyl bromides vs. iodides) were also studied...
December 26, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27976495/detection-of-dna-double-strand-breaks-by-pulsed-field-gel-electrophoresis
#10
Yuri Kawashima, Nahomi Yamaguchi, Rie Teshima, Hisashi Narahara, Yoshio Yamaoka, Hirofumi Anai, Yoshihiro Nishida, Katsuhiro Hanada
A DNA double-strand break (DSB) is one of the most cytotoxic DNA lesions because unrepaired DSBs cause chromosomal aberrations and cell death. Although many physiological DSBs occur at DNA replication sites, the molecular mechanisms underlying this remain poorly understood. There was therefore a need to develop a highly specific method to detect DSB fragments containing DNA replication sites. Here we investigated whether pulsed-field gel electrophoresis (PFGE) combined with visualization of DNA replication sites by immunoblotting using halogenized deoxyuridines, such as BrdU and IdU, was sufficient for this detection...
January 2017: Genes to Cells: Devoted to Molecular & Cellular Mechanisms
https://www.readbyqxmd.com/read/27934403/transition-metal-complex-cationic-dyes-photosensitive-to-two-types-of-2d-layered-silver-bromides-with-visible-light-driven-photocatalytic-properties
#11
Cheng-Yang Yue, Xiao-Wu Lei, Yong-Fang Han, Xin-Xiu Lu, Ya-Wei Tian, Jing Xu, Xiao-Fan Liu, Xin Xu
With mixed transition-metal (TM) complex, alkali-metal cations, or halogen anions as structure-directing agents, two types of two-dimensional (2D) layered inorganic-organic hybrid silver bromides were prepared and structurally characterized as K[TM(2,2-bipy)3]2Ag6Br11 (TM = Ni (1), Co (2), Zn (3), Fe (4)) and [TM(2,2-bipy)3]2Ag13Br17 (TM = Ni (5), Co (6), Zn (7), Fe (8)). Compounds 1-4 feature 2D microporous anionic [Ag6Br11](5-) layers composed of [Ag3Br7] secondary building units based on AgBr4 tetrahedral units, and compounds 5-8 contain 2D [Ag13Br16](3-) layers built from the one-dimensional complex [Ag8Br12] and [Ag5Br8] chains...
December 5, 2016: Inorganic Chemistry
https://www.readbyqxmd.com/read/27931386/fate-of-environmental-pollutants
#12
Lokesh P Padhye
This annual review covers the literature published in 2015 on topics related to the occurrence and fate of emerging environmental pollutants in wastewater. Due to the vast amount of literature published on this topic, I have discussed only a fraction of the quality research publications, up to maximum 20 relevant articles per section, due to limitation of space. The abstract search was carried out using Web of Science, and the abstracts were selected based on their relevance. In few cases, full-text articles were referred to better understand new findings...
October 2016: Water Environment Research: a Research Publication of the Water Environment Federation
https://www.readbyqxmd.com/read/27898256/comparative-study-of-the-physiotherapeutic-and-drug-protocol-and-low-level-laser-irradiation-in-the-treatment-of-pain-associated-with-temporomandibular-dysfunction
#13
Marcos Fernando Xisto Braga Cavalcanti, Uoston Holder Silva, Ernesto Cesar Pinto Leal-Junior, Rodrigo A B Lopes-Martins, Rodrigo Labat Marcos, Rodney Capp Pallotta, Francesca Diomede, Oriana Trubiani, Natalia De Isla, Lucio Frigo
BACKGROUND: The temporomandibular joint (TMJ) is a structure of the craniofacial complex affected by neurological diseases. Orthopedic and musculoskeletal changes can also cause temporomandibular disorders (TMD) and pain. Low-level laser (LLL) therapy has been studied in the treatment of temporomandibular jaw (TMJ) dysfunction, and controversial results were obtained. OBJECTIVE: The objective of this work was comparing the physiotherapeutic and drug protocol (PDP) to LLL therapy in the treatment of pain associated with TMD...
December 2016: Photomedicine and Laser Surgery
https://www.readbyqxmd.com/read/27892835/effect-of-adhesive-restoration-and-bleaching-technique-on-the-concentration-of-hydrogen-peroxide-in-the-pulp-chamber
#14
V Cavalli, B G Silva, S B Berger, G Abuna, F C Marson, Cpm Tabchoury, M Giannini
This study aimed to quantify the concentration of hydrogen peroxide into the pulp chamber in the presence or absence of adhesive enamel restorations and to analyze the resin-dentin interface of bleached groups. Bovine incisors (120) were randomly divided into three groups according to enamel treatment (n=40 each): (1) enamel without restoration (control); (2) enamel cavities (3 mm diameter × 1.5 mm depth) restored with a silorane-based (SB) system; or (3) enamel cavities (3 mm diameter × 1.5 mm depth) restored with a dimethacrylate-based (DB) system...
November 28, 2016: Operative Dentistry
https://www.readbyqxmd.com/read/27892815/monitoring-trihalomethanes-and-nitrogenous-disinfection-by-products-in-blending-desalinated-waters-using-solid-phase-microextraction-and-gas-chromatography
#15
Providencia González-Hernández, Manuel Hernández-Padrón, Verónica Pino, Ana M Afonso, Juan H Ayala
A simple and efficient method has been developed for the extraction and determination of 16 common volatile halogenated disinfection by-products (DBPs) (four trihalomethanes, six haloacetonitriles, and six halonitromethanes) in blending desalinated waters, using headspace solid-phase microextraction and gas chromatography with flame ionization detector (HS-SPME/GC-FID). After the optimization using factorial designs of the HS-SPME parameters (optimum: carboxen/polydimethylsiloxane such as fiber, extraction time of 60 min at 30°C, pH 7, addition of 40% (w/v) of sodium chloride, and desorption time of 2 min at 250°C), quantification limits ranged from 3...
December 14, 2016: Environmental Technology
https://www.readbyqxmd.com/read/27868274/apci-as-an-innovative-ionization-mode-compared-to-ei-and-ci-for-the-analysis-of-a-large-range-of-organophosphate-esters-using-gc-ms-ms
#16
Wafaa Halloum, Ronan Cariou, Gaud Dervilly-Pinel, Farouk Jaber, Bruno Le Bizec
Organophosphate esters (OPEs) are chemical compounds incorporated into materials as flame-proof and/or plasticizing agents. In this work, 13 non-halogenated and 5 halogenated OPEs were studied. Their mass spectra were interpreted and compared in terms of fragmentation patterns and dominant ions via various ionization techniques (electron ionization (EI) and chemical ionization (CI) under vacuum and corona discharge atmospheric pressure chemical ionization (APCI)) on gas chromatography coupled to mass spectrometry (GC-MS)...
November 21, 2016: Journal of Mass Spectrometry: JMS
https://www.readbyqxmd.com/read/27825064/oxidized-carbo-iron-causes-reduced-reproduction-and-lower-tolerance-of-juveniles-in-the-amphipod-hyalella-azteca
#17
Mirco Weil, Tobias Meißner, Armin Springer, Mirco Bundschuh, Lydia Hübler, Ralf Schulz, Karen Duis
For in situ remediation of groundwater contaminated by halogenated hydrocarbons Carbo-Iron(®), a composite of microscale activated carbon and nano Fe(0), was developed. Against the background of intended release of Carbo-Iron into the environment in concentrations in the g/L-range, potential ecotoxicological consequences were evaluated in the present study. The nano Fei(0) in Carbo-Iron acts as reducing agent and is oxidized in aqueous systems by chlorinated solvents, groundwater constituents (e.g. dissolved oxygen) and anaerobic corrosion...
December 2016: Aquatic Toxicology
https://www.readbyqxmd.com/read/27775033/new-insecticidal-agents-from-halogenation-acylation-of-the-furyl-ring-of-fraxinellone
#18
Yong Guo, Ruige Yang, Hui Xu
Introduction of the halogen atom or the acyl group at the C-ring of fraxinellone was investigated. Some unexpected halogenation products were obtained with the different chlorination/bromination reagents, and their possible reaction mechanisms were also proposed. Seven key steric structures of 2a', 2b, 2b', 2c', 3a, 3b, and one isomer (5'α-Cl) of 2a were further confirmed by single-crystal X-ray diffraction. Especially compounds 2a, 2a', 3a and 3c exhibited more potent insecticidal activity than toosendanin...
October 24, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27750147/synthesis-and-evaluation-of-halogenated-12n-sulfonyl-matrinic-butanes-as-potential-anti-coxsackievirus-agents
#19
Xin-Yue Cheng, Yu-Huan Li, Sheng Tang, Xin Zhang, Yan-Xiang Wang, Sheng-Gang Wang, Jian-Dong Jiang, Ying-Hong Li, Dan-Qing Song
Twenty-eight new 12N-benzenesulfonyl matrinic butane and halogenated 12N-sulfonyl matrinic butane/ethane derivatives were designed, synthesized and evaluated for their anti-coxsakievirus activities against CVB3 taking compound 1 as the lead. SAR analysis indicated the introduction of a fluoro atom on the 1'-position might be helpful for keeping potency. Among them, compound 8a exhibited potential activities against all CVBs with IC50 ranging from 0.69 to 5.14 μM, suggesting a broad-spectrum anti-coxsackievirus B feature...
September 30, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27727486/monomeric-cinchona-alkaloid-based-catalysts-for-highly-enantioselective-bromolactonisation-of-alkynes
#20
Michael Wilking, Constantin G Daniliuc, Ulrich Hennecke
The cinchona alkaloid dimer (DHQD)2 PHAL has been shown to be a broadly applicable catalyst for asymmetric halogenations. However, this catalyst does not have to be dimeric and a class of monomeric quinidine and quinine-derived catalysts was prepared, often showing superior selectivity in bromolactonisations of terminal alkynoic acids. Mechanistic investigations show that these organocatalysts act as host molecules that can bind carboxylic acid-based substrates as guests with substantial binding constants. Based on these findings, it is proposed that this class of catalysts is bifunctional in nature activating the halogenating agent as well as the nucleophile in electrophilic halogenation reactions...
December 19, 2016: Chemistry: a European Journal
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