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61.
Dr. Dimitra T. Pournara Anna Durner Dr. Eftichia Kritsi Alexios Papakostas Dr. Panagiotis Zoumpoulakis Prof. Dr. Annette Nicke Dr. Maria Koufaki 《ChemMedChem》2020,15(24):2530-2543
The P2X7 receptor is a promising target for the treatment of various diseases due to its significant role in inflammation and immune cell signaling. This work describes the design, synthesis, and in vitro evaluation of a series of novel derivatives bearing diverse scaffolds as potent P2X7 antagonists. Our approach was based on structural modifications of reported (adamantan-1-yl)methylbenzamides able to inhibit the receptor activation. The adamantane moieties and the amide bond were replaced, and the replacements were evaluated by a ligand-based pharmacophore model. The antagonistic potency of the synthesized analogues was assessed by two-electrode voltage clamp experiments, using Xenopus laevis oocytes that express the human P2X7 receptor. SAR studies suggested that the replacement of the adamantane ring by an aryl-cyclohexyl moiety afforded the most potent antagonists against the activation of the P2X7 cation channel, with analogue 2-chloro-N-[1-(3-(nitrooxymethyl)phenyl)cyclohexyl)methyl]benzamide ( 56 ) exhibiting the best potency with an IC50 value of 0.39 μM. 相似文献
62.
为总结出一套适合矿山实际的支护方案,二里河铅锌矿在矿山生产的20余年里,引进了多种支护工艺进行试验。矿山根据井巷、硐室所处工程环境,确定了锚杆、钢筋、钢架、混凝土进行单一或组合支护的方案,特别是千枚岩内12.4 m跨度的提升机硐室支护方式与参数,对矿山软弱岩层大跨度硐室工程支护具有参考价值。采场则按照急倾斜、缓倾斜矿体上盘千枚岩支护为例,分别列举了锚杆、锚杆+锚索支护的工程方案。采场联络巷、矿房行人通道等区域利用支柱+横梁临时支护。不但提高了采场作业安全性,也使采矿损失率降低5%,贫化率降低7%。 相似文献
63.
《Ceramics International》2020,46(13):20974-20984
Photocatalytic technology is an environmentally safe method of eliminating organic pollutants and antibiotics in wastewater. In this research, the performance of Fe3O4/CdS/g-C3N4 (FCN) photocatalyst for degradation of antibiotics was studied. The composite photocatalysts with different concentrations of g-C3N4 were prepared. FCN has better photocatalytic activity than degradation dyes in removal of antibiotics under visible light. This indicates that FCN could effectively hinder the recombination of carriers, and the addition of g-C3N4 increases the optical response range of CdS. At the same time, the introduction of Fe3O4 magnetic nanoparticles overcomes the problem of difficulty in recovery of the powder photocatalyst. The photocatalytic activity is not reduced to any significant after three cycles of use. 相似文献
64.
65.
采用水热法制备双钙钛矿催化剂Sr_2FeNiO_6,考察不同浓度KOH溶液(4 mol·L~(-1)、6 mol·L~(-1)、8 mol·L~(-1)、10 mol·L~(-1)、12 mol·L~(-1)、14 mol·L~(-1))对催化剂性能的影响,利用X射线衍射、比表面积测定、程序升温还原和扫描电镜等对样品进行性能表征,并以催化甲烷燃烧为目标,考察催化剂催化性能。结果表明,矿化剂KOH浓度对样品性能影响较大,当浓度为10 mol·L~(-1)时,起燃温度最低,T_(10%)为430℃;浓度为8 mol·L~(-1)时,样品比表面积最大,为19.0 m~2·g~(-1),完全燃烧温度最低,T_(90%)为610℃。 相似文献
66.
Ahlam Ammar Sharif 《建筑学研究前沿(英文版)》2020,9(4):837-857
Urban researchers have maintained a constant interest in the complexity and continuity of urban space usage. Some have applied actor–network theory (ANT) to investigate the heterogeneity of spaces and present them through the networks of their users’ activities. However, these accounts are predominantly limited in examining the extent to which these spaces may be heterogeneous when exploring such networks. This paper draws on recent ANT scholarship, which employs an ethnographic research conducted in a main park in a housing project at Dahiyat Al Hussein in Amman, Jordan. The findings describe the complex and unpredictable negotiations that occur within spaces by documenting the varieties and interrelations among user activity networks within this common and shared urban space. This research reveals the extent to which spaces, parks in this case, may be heterogeneous by unpacking their usage. The conclusions and insights assert the necessity of paying attention to design detail and creating designs that are responsive to evolving user activities. 相似文献
67.
离子液体是近年来发展起来的一种绿色介质,在化工反应和分离过程中具有广泛的应用前景。离子液体的溶液热力学性质和相平衡数据是其相关工艺过程设计的基础。本文从如下几个方面综述了离子液体溶液热力学模型的研究进展,即溶液热力学研究方法、溶液热力学模型的构建、离子液体的结构和分子间作用力、离子液体的溶液热力学模型及其在相平衡计算中的应用。重点分析了适用于离子液体溶液热力学性质计算的状态方程模型和过量Gibbs自由能模型或活度系数模型,离子液体的电解质和非电解质溶液模型,以及这些模型对ILs结构、氢键和静电作用的处理方法。分析了这些模型的优缺点,并对今后离子液体的溶液热力学研究提出了建议。 相似文献
68.
María Clara Verdi Constanza Melian Patricia Castellano Graciela Vignolo Mariana Blanco Massani 《International Journal of Food Science & Technology》2020,55(1):267-275
The effectiveness of antimicrobial mixtures against Listeria innocua 7, used as a L. monocytogenes surrogate, was investigated in broth and a food system. Synergistic effects were found for nisin (Nis), potassium sorbate (PS), calcium propionate (CP) and sodium lactate (SL), Nis + PS being the most effective binary mixture that exhibited listericidal activity in broth. To assess the effect of adding lactocin AL705 (AL705) to Nis + organic acid salt combinations, tridimensional isobolograms were generated. Sub-MIC combinations of the antimicrobials exerted bactericidal activity against L. innocua 7 after AL705 addition to the binary mixtures. However, when applied on Sardo cheese contaminated with L. innocua 7 (initial inoculum 4.45 ± 0.06 CFU g−1), only Nis + PS + AL705 produced count reductions respect to the control, reaching 3.04 ± 0.35 CFU g−1 counts after 15 days at 15 °C. Ternary combinations containing AL705 showed potential to reduce antimicrobial usages for L. innocua 7 inhibition. 相似文献
69.
Jorge Pascual-Fernndez Alejandro Fernndez-Montero Alfredo Crdova-Martínez Diego Pastor Alejandro Martínez-Rodríguez Enrique Roche 《International journal of molecular sciences》2020,21(22)
Aging is associated with sarcopenia. The loss of strength results in decreased muscle mass and motor function. This process accelerates the progressive muscle deterioration observed in older adults, favoring the presence of debilitating pathologies. In addition, sarcopenia leads to a decrease in quality of life, significantly affecting self-sufficiency. Altogether, these results in an increase in economic resources from the National Health Systems devoted to mitigating this problem in the elderly, particularly in developed countries. Different etiological determinants are involved in the progression of the disease, including: neurological factors, endocrine alterations, as well as nutritional and lifestyle changes related to the adoption of more sedentary habits. Molecular and cellular mechanisms have not been clearly characterized, resulting in the absence of an effective treatment for sarcopenia. Nevertheless, physical activity seems to be the sole strategy to delay sarcopenia and its symptoms. The present review intends to bring together the data explaining how physical activity modulates at a molecular and cellular level all factors that predispose or favor the progression of this deteriorating pathology. 相似文献
70.
The microstructure and electrochemical behavior of Mg–6Al–1Zn, Mg–6Al–1Zn–1Ga, Mg–6Al–1Zn–1Sn, and Mg–6Al–1Zn–0.5Sn–0.5Ga as anode materials in a 3.5 wt% NaCl solution are compared systematically. The results show that Sn alloying refines the second-phases of Mg–6Zn–1Al by promoting tiny granular Mg17Al12 phases containing Sn, and inspires their disperse distribution. However, the Ga results in the formation of semicontinuous reticular Ga containing Mg17Al12 phases. The comparison of discharge tests indicates that Mg–6Al–1Zn–1Sn has the highest discharge activity, and Mg–6Al–1Zn–1Ga displays the largest hydrogen evolution corrosion resistance in 3.5 wt% NaCl solution at 298 K. The synergy of Ga and Sn can shorten discharge activation time and promote low discharge potential. In addition, the utilization efficiencies of the alloys decrease as follows: Mg–6Al–1Zn–1Ga > Mg–6Al–1Zn–0.5Sn–0.5Ga > Mg–6Al–1Zn–1Sn > Mg–6Zn–1Al. This study illustrates that the Mg–6Al–1Zn–0.5Sn–0.5Ga alloy has acceptable utilization efficiency and desirable electrochemical activity, which implies that doping Ga and Sn obtains a balance between discharge activity and utilization efficiencies. 相似文献