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排序方式: 共有1094条查询结果,搜索用时 31 毫秒
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Dr. Elena Petit Dr. Lluís Bosch Prof. Anna M. Costa Ignacio Rodríguez-Izquierdo Dr. Daniel Sepúlveda-Crespo Prof. M. Angeles Muñoz-Fernández Prof. Jaume Vilarrasa 《ChemMedChem》2021,16(14):2217-2222
Amides from indole-3-glyoxylic acid and 4-benzoyl-2-methylpiperazine, which are related to entry inhibitors developed by Bristol-Myers Squibb (BMS), have been synthesized with aliphatic chains located at the C7 position of the indole ring. These spacers contain an azido group suitable for the well-known Cu(I)-catalyzed (3+2)-cycloaddition or an activated triple bond for the nucleophilic addition of thiols under physiological conditions. Reaction with polyols (β-cyclodextrin and hyperbranched polyglycerol) decorated with complementary click partners has afforded polyol-BMS-like conjugates that are not cytotoxic (TZM.bl cells) and retain the activity against R5-HIV-1NLAD8 isolates. Thus, potential vaginal microbicides based on entry inhibitors, which can be called of 4th generation, are reported here for the first time. 相似文献
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Ren A Hauyon Gabriela Garrido‐Gatica Patricio A Sobarzo Carmen M Gonzlez‐Henríquez Luis H Tagle Fidel E Rodríguez‐Gonzlez Ignacio A Jessop Gonzalo Recabarren‐Gajardo Alain Tundidor‐Camba Claudio A Terraza 《Polymer International》2020,69(3):239-247
Aromatic poly(azomethine)s have been studied due to their attractive properties such as high thermal stability, semiconducting behavior and the ability to coordinate species with their imine units (C?N). In this paper, the synthesis and characterization of two novel silylated poly(azomethine)s containing cardo units are reported. These materials were highly soluble in organic solvents such as chloroform and m‐cresol and were thermally stable, and PAzMC1 exhibited a high glass transition temperature value (287 °C), while that for PAzMC2 was not observed. UV–visible spectrophotometry revealed absorption bands related to the aromatic backbone of both PAzMCs, 300–285 nm in tetrahydrofuran and 310–301 nm in dimethylsulfoxide, and bands attributed to the conjugated imine unit at around 350 nm. In order to investigate the phenomenon of the emission of fluorescence promoted by dopant agents with regard to potential optoelectronic applications, the materials were doped with H2SO4 and their optical and electrochemical properties investigated. Thus, the absorption band of the imine group was suppressed due to the nitrogen atoms being protonated. Fluorescence spectroscopy analysis developed in dilute solutions of polymers showed no emission from the undoped polymers, whereas the acid‐doped species emitted fluorescence in the UV and violet regions (322 nm). Cyclic voltammetry measurements were carried out and HOMO–LUMO energies were estimated. This study provides a starting point for the development of new poly(azomethine)s with doping‐dependent emission. © 2019 Society of Chemical Industry 相似文献
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Ana Carolina Ruberte Gustavo Gonzlez-Gaitano Arun K. Sharma Carlos Aydillo Ignacio Encío Carmen Sanmartín Daniel Plano 《International journal of molecular sciences》2020,21(23)
Aspirin (ASA) has attracted wide interest of numerous scientists worldwide thanks to its chemopreventive and chemotherapeutic effects, particularly in colorectal cancer (CRC). Incorporation of selenium (Se) atom into ASA has greatly increased their anti-tumoral efficacy in CRC compared with the organic counterparts without the Se functionality, such as the promising antitumoral methylseleno-ASA analog (1a). Nevertheless, the efficacy of compound 1a in cancer cells is compromised due to its poor solubility and volatile nature. Thus, 1a has been formulated with native α-, β- and γ-cyclodextrin (CD), a modified β-CD (hydroxypropyl β-CD, HP-β-CD) and Pluronic F127, all of them non-toxic, biodegradable and FDA approved. Water solubility of 1a is enhanced with β- and HP- β-CDs and Pluronic F127. Compound 1a forms inclusion complexes with the CDs and was incorporated in the hydrophobic core of the F127 micelles. Herein, we evaluated the cytotoxic potential of 1a, alone or formulated with β- and HP- β-CDs or Pluronic F127, against CRC cells. Remarkably, 1a formulations demonstrated more sustained antitumoral activity toward CRC cells. Hence, β-CD, HP-β-CD and Pluronic F127 might be excellent vehicles to improve pharmacological properties of organoselenium compounds with solubility issues and volatile nature. 相似文献
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Ismael Pérez Ignacio Moreno-Ventas Guillermo Ríos 《International Journal of Applied Ceramic Technology》2020,17(2):625-636
A cost driver in the copper-making industry is the periodical relining of the furnaces because of wear. This paper presents thermochemical calculations (using the FactSage™ database) focused on the evaluation of the slag-refractory chemical interaction in a submerged arc furnace (SAF) used for slag-cleaning operations. This evaluation was made under different conditions: slag-refractory volume ratio, oxygen partial pressure, and different types of slag. The new phases formed as a consequence of the slag-refractory chemical interaction were identified and quantified. To support the theoretical calculations based on thermochemistry, a postmortem study was carried out on a SAF used at the Atlantic Copper Smelter (Spain) after a 6-year campaign (4.5 mill. t. slag processed). Refractory samples were taken from different locations on the wall and analyzed using a scanning electron microscope equipped with an Energy Dispersive Spectroscopy system. 相似文献
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Victor Otero-Tuárez Idoya Fernández-Pan Juan Ignacio Maté 《International Journal of Food Science & Technology》2020,55(5):2113-2121
Physical, chemical and antimicrobial properties of fish gelatin films with different concentrations of ethyl lauroyl arginate (LAE) were studied. Optical properties of film-forming solution did not vary with increased LAE content. However, pH and surface tension increased. The incorporation of LAE into the formulation increased moisture and solubility of the films. In addition, the presence of LAE affected mechanical properties, making films stronger and more flexible; it had no effect on water vapour permeability. Finally, films with LAE significantly increased antimicrobial properties against Listeria innocua, Shewanella putrefaciens and Pseudomonas fluorescens, but not against Aeromonas hydrophila. These antimicrobial films could be used as an alternative technology for extending shelf-life of fresh fish products. 相似文献
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