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排序方式: 共有1492条查询结果,搜索用时 375 毫秒
1.
Dr. Maria L. Di Paolo Dr. Michael S. Christodoulou Dr. Alessandra M. Calogero Dr. Luca Pinzi Prof. Giulio Rastelli Prof. Daniele Passarella Prof. Graziella Cappelletti Prof. Lisa Dalla Via 《ChemMedChem》2019,14(18):1641-1652
A series of 2-phenyloxazoles bearing an amide group at position 4 were designed and synthesized for evaluation as potential inhibitors of human recombinant monoamine oxidases (hrMAOs). Results of kinetics experiments demonstrated that all compounds behave as competitive MAO inhibitors, with good selectivity toward the MAO-B isoform. The most potent and selective derivatives are characterized by inhibition constant (Ki) values in the sub-micromolar range and a good selectivity index (Ki MAO-A/Ki MAO-B>50). Some derivatives were also found to be able to inhibit MAO activity in nerve growth factor (NGF)-differentiated PC12 cells, taken as a model of neuronal cells. In particular, 2-(2-hydroxyphenyl)-N-phenyloxazole-4-carboxamide (compound 4 a ) may be a promising new scaffold, exerting the highest selectivity and inhibitory effect toward MAOs in NGF-differentiated PC12 cell lysates, without compromising cell viability. Molecular docking analysis allowed a rationalization of the experimentally observed binding affinity and selectivity. 相似文献
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The physical gestures that operate music instruments are responsible for the qualities of the sound being produced in a performance.
Gestural information is thereby crucial for a model of music performance, paired with a model of sound synthesis where this
information is applied. The highly constrained nature of performers gestures makes this task suitable to be modeled via a
constraint-based approach, coupled with a strategy aimed at maximizing the gestural comfort of performers. We illustrate the
problem representation, the search strategy and a validation of the model against human performance. 相似文献
4.
Two different Ti/Pt–Ir materials (commercial and home made) and Ti/PdO + Co3O4 were investigated for their electrocatalytic properties versus Cl2 evolution reaction. The materials were used in a batch electrochemical reactor to treat biologically recalcitrant di-azo compound. An electrochemically driven oxidation, mediated by a Cl2/Cl− couple, proved efficient for destruction of this complex organic molecule, causing cleavage of the conjugated double bonds and destruction of unsatured bonds. Both Ti/Pt–Ir materials performed well; lower kinetics obtained with the Ti/PdO + Co3O4 anode was caused by adsorption of the model compound, evidenced in preliminary voltammetric measurements. The dye oxidation reaction followed the second order kinetics with partial orders in the model compound and (time varying) chlorine concentrations equal to one. Specific energy consumption of 3.12 kWh m−3 proved the process more economic than the homogeneous phase oxidation. 相似文献
5.
In this paper, two brittle fracture problems are numerically simulated: the failure of a ceramic ring under centrifugal loading and crack branching in a PMMA strip. A three‐dimensional finite element package in which cohesive elements are dynamically inserted has been developed. The cohesive elements' strength is chosen to follow a modified weakest link Weibull distribution. The probability of introducing a weak cohesive element is set to increase with the cohesive element size. This reflects the physically based effect according to which larger elements are more likely to contain defects. The calculations illustrate how the area dependence of the Weibull model can be used to effectively address mesh dependency. On the other hand, regular Weibull distributions have failed to reduce mesh dependency for the examples shown in this paper. The ceramic ring calculations revealed that two distinct phenomena appear depending on the magnitude of the Weibull modulus. For low Weibull modulus, the fragmentation of the ring is dominated by heterogeneities. Whereas many cracks were generated, few of them could propagate to the outer surface. Monte Carlo simulations revealed that for highly heterogeneous rings, the number of small fragments was large and that few large fragments were generated. For high Weibull modulus, signifying that the ring is close to being homogeneous, the fragmentation process was very different. Monte Carlo simulations highlighted that a larger number of large fragments are generated due to crack branching. Copyright © 2003 John Wiley & Sons, Ltd. 相似文献
6.
In this work, a possible way for partial CO2 emissions reduction from gas turbine exhausts by co-firing with biomass is investigated. The basic principle is the recirculation of a fraction of the exhausts (still rich in oxygen) to a gasifier, in order to produce syngas to mix with natural gas fuel. As biomass is a CO2 neutral fuel, the fraction of replaced natural gas is a measure of CO2 removal potential of the powerplant. 相似文献
7.
We report measurements of the specific heat of thin helium films adsorbed in the 0.2 µm pores of Anopore membranes. Over the temperature range of these studies, two specific heat anomalies, strongly dependent on helium film thickness, were found. 相似文献
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Unilateral spatial neglect declines when participants reach to grip the center of long metal rods compared with when they point to the perceived center, suggesting that visuomotor control systems are less affected by neglect than other representational systems (I. H. Robertson, D. Nico, & B. Hood, 1995). In this study, 16 participants with unilateral left neglect actually picked up rods, and we predicted short-term improvements in neglect because of induced conflict between a phenomenally symmetrical visual world on the one hand and a proprioceptively conveyed rightward-biased world on the other. With participants serving as their own controls, significant short-term improvements in neglect were found on 2 out of 4 neglect tasks after participants experienced proprioceptive feedback discrepant from the judgments they made on the basis of visual information alone. (PsycINFO Database Record (c) 2010 APA, all rights reserved) 相似文献
10.
G. Straffelini A. Molinari D. Trabucco 《Metallurgical and Materials Transactions A》2002,33(3):613-624
The dry sliding behavior of a 304L austenitic stainless steel and a duplex 2205 austenitic-ferritic stainless was investigated.
The evolution of wear was characterized by the existence of a sliding-distance transition. In particular, wear passed from
delamination to tribo-oxidation, with a reduction in wear rate. The occurrence of such a transition was interpreted with reference
to a theory of sliding wear based on the formation, by subsurface plastic deformation, of a tribological layer and its detachment
during sliding. It has been found that the transition is controlled by the ability of the tribological system to form, on
its outer part, a protective oxide-rich scale. This introduces a kinetic limitation, which is particularly important in the
case of the duplex 2205, because of its lower ductility in comparison to the 304L steel. In this frame, the influence of sliding
velocity, the particular frictional behavior, the role of chromium in the oxidative wear, and the surface temperature evolution
during sliding could be explained. 相似文献