排序方式: 共有37条查询结果,搜索用时 0 毫秒
1.
Novel Tacrine‐Grafted Ugi Adducts as Multipotent Anti‐Alzheimer Drugs: A Synthetic Renewal in Tacrine–Ferulic Acid Hybrids 下载免费PDF全文
Mohamed Benchekroun Dr. Manuela Bartolini Dr. Javier Egea Dr. Alejandro Romero Dr. Elena Soriano Dr. Marc Pudlo Vincent Luzet Prof. Vincenza Andrisano Dr. María‐Luisa Jimeno Dr. Manuela G. López Sarah Wehle Prof. Tijani Gharbi Prof. Bernard Refouvelet Lucía de Andrés Clara Herrera‐Arozamena Prof. Barbara Monti Prof. Maria Laura Bolognesi Prof. María Isabel Rodríguez‐Franco Prof. Dr. Michael Decker Prof. José Marco‐Contelles Dr. Lhassane Ismaili 《ChemMedChem》2015,10(3):523-539
Herein we describe the design, multicomponent synthesis, and biological, molecular modeling and ADMET studies, as well as in vitro PAMPA‐blood–brain barrier (BBB) analysis of new tacrine–ferulic acid hybrids (TFAHs). We identified (E)‐3‐(hydroxy‐3‐methoxyphenyl)‐N‐{8[(7‐methoxy‐1,2,3,4‐tetrahydroacridin‐9‐yl)amino]octyl}‐N‐[2‐(naphthalen‐2‐ylamino)2‐oxoethyl]acrylamide (TFAH 10 n ) as a particularly interesting multipotent compound that shows moderate and completely selective inhibition of human butyrylcholinesterase (IC50=68.2 nM ), strong antioxidant activity (4.29 equiv trolox in an oxygen radical absorbance capacity (ORAC) assay), and good β‐amyloid (Aβ) anti‐aggregation properties (65.6 % at 1:1 ratio); moreover, it is able to permeate central nervous system (CNS) tissues, as determined by PAMPA‐BBB assay. Notably, even when tested at very high concentrations, TFAH 10 n easily surpasses the other TFAHs in hepatotoxicity profiling (59.4 % cell viability at 1000 μM ), affording good neuroprotection against toxic insults such as Aβ1–40, Aβ1–42, H2O2, and oligomycin A/rotenone on SH‐SY5Y cells, at 1 μM . The results reported herein support the development of new multipotent TFAH derivatives as potential drugs for the treatment of Alzheimer′s disease. 相似文献
2.
We introduced recently phase measurements usually performed in interferometry to the domain of image processing and intelligent vision [IEEE Trans. Instrum. Meas. 49, 867 (2000)]. Our purpose is to sense with a high accuracy the position, orientation, and displacement of two-dimensional (2D) surfaces observed by a static vision system. We report on significant improvements of the method. Experimental measurements reveal a peak-valley noise of approximately 10(-2) CCD pixel, corresponding approximately to a 10(-3) period of the phase reference pattern. Then the observation of 10 microm scaled features enables an accuracy of a few nm in the position sensing of the phase reference pattern for the extended 2D measurement range. 相似文献
3.
We study in this paper the capacity of the downlink of OFDMA-based IEEE802.16 WiMAX system in the presence of two types of traffic, streaming and elastic. We focus in particular on the impact of Adaptive Modulation and Coding (AMC) as well as inter-cell interference resulting from different frequency reuse schemes. Several performance measures, namely blocking rates, mean transfer time and the mean number of collisions between two OFDMA WiMAX cells, are then derived and quantified. We show that reuse partitioning results in a higher blocking rate at the appreciable gain in terms of lower mean transfer time for users close to the base station as well as a lower number of collisions which implies a higher throughput. 相似文献
4.
We propose and study a new set of enhancement features to improve the performance of reliable transport in Delay Tolerant Networks (DTNs) consisting of both unicast and multicast flows. The improvement in reliability is brought in by a novel Global Selective ACKnowledgment (G-SACK) scheme and random linear network coding. The motivation for using network coding and G-SACKs comes from the observation that one should take the maximum advantage of the contact opportunities which occur quite infrequently in DTNs. Network coding and G-SACKs perform “mixing” of packet and acknowledgment information, respectively, at the contact opportunities and essentially solve the randomness and finite capacity limitations of DTNs. In contrast to earlier work on network coding in DTNs, we observe and explain the gains due to network coding even under an inter-session setting. Our results from extensive simulations of appropriately chosen “minimal” topologies quantify the gains due to each enhancement feature. We show that substantial gains can be achieved by our proposed enhancements that are very simple to implement. 相似文献
5.
The thermodynamics modeling of a Reiner–Philippoff-type fluid is essential because it is a complex fluid with three distinct probable modifications. This fluid model can be modified to describe a shear-thinning, Newtonian, or shear-thickening fluid under varied viscoelastic conditions. This study constructs a mathematical model that describes a boundary layer flow of a Reiner–Philippoff fluid with nonlinear radiative heat flux and temperature- and concentration-induced buoyancy force. The dynamical model follows the usual conservation laws and is reduced through a nonsimilar group of transformations. The resulting equations are solved using a spectral-based local linearization method, and the accuracy of the numerical results is validated through the grid dependence and convergence tests. Detailed analyses of the effects of specific thermophysical parameters are presented through tables and graphs. The study reveals, among other results, that the buoyancy force, solute and thermal expansion coefficients, and thermal radiation increase the overall wall drag, heat, and mass fluxes. Furthermore, the study shows that amplifying the space and temperature-dependent heat source parameters allows fluid particles to lose their cohesive force and, consequently, maximize flow and heat transfer. 相似文献
6.
Tijanić Ksenija Car-Pušić Diana Šperac Marija 《Neural computing & applications》2020,32(13):9343-9355
Neural Computing and Applications - Road construction projects on the territory of the Republic of Croatia are characterized by the overrun of planned costs. The experience of the contractor on... 相似文献
7.
Through the variation of their cross sections, the in vivo response of lower back muscles to low loading in an upright seated posture is explored by the Fourier-transform profilometry technique. The maximization of its sensitivity allows us to reach an adequate resolution for the evaluation of low-back displacements. Refinements of the fringe pattern analysis permit the minimization of errors. The experiments show an asymmetric distribution of the displacement during head rotation movements. Significant contribution of the lower back to grasping exertions is also observed. These results are thought to be useful for early defect detection in the lower back. 相似文献
8.
One way to extend depth of field of any optical system is to take several images with different focus positions and combine them into a single composite image, which contains all regions fully focused. The challenge then becomes to select from each image the pixels that are in focus. We describe a new focus measure based on the shapelet decomposition. Results using simulated images with high noise content show that the shapelet-based focus measure is the most performance that traditional neighborhood-based focus approaches. Similarly shapelet focus measure provides significant improvement compared to traditional methods when objects have nontextured or homogeneous regions. 相似文献
9.
Anis Jdidi Tijani Chahed Salah Eddine Elayoubi Hichem Besbes 《Telecommunication Systems》2012,50(3):169-180
Hierarchical Modulation (HM) is a means to enhance the spectral efficiency of a system by superposing, in terms of modulation, an additional stream for a given user with good radio conditions on a basic stream of a user with worse radio conditions. This, in turn, increases the throughput of the former user and hence the overall performance of the whole system. We consider, in this work, such a performance at the flow level, for a realistic dynamic setting where users come to the system and leave it after a finite duration corresponding, for instance, to the completion of a file transfer. We specifically model and quantify, both analytically and via simulations, the gain thus achieved and propose two extensions to the basic HM algorithm: a first one in which a user with bad radio conditions is also superposed on one with better radio conditions and a second one in which a user of one type is further superposed on a user of the same type as well. 相似文献
10.
Phase-unwrapping algorithm for images with high noise content based on a local histogram 总被引:2,自引:0,他引:2
We present a robust algorithm of phase unwrapping that was designed for use on phase images with high noise content. We proceed with the algorithm by first identifying regions with continuous phase values placed between fringe boundaries in an image and then phase shifting the regions with respect to one another by multiples of 2pi to unwrap the phase. Image pixels are segmented between interfringe and fringe boundary areas by use of a local histogram of a wrapped phase. The algorithm has been used successfully to unwrap phase images generated in a three-dimensional shape measurement for noninvasive quantification of human skin structure in dermatology, cosmetology, and plastic surgery. 相似文献