排序方式: 共有46条查询结果,搜索用时 15 毫秒
1.
scar M. Bautista‐Aguilera Lhassane Ismaili Isabel Iriepa Daniel Diez‐Iriepa Fakher Chabchoub Jos Marco‐Contelles Marta Prez 《Chemical record (New York, N.Y.)》2021,21(1):162-174
Herein we have reviewed our recent developments for the identification of new tacrine analogues for Alzheimer's disease (AD) therapy. Tacrine, the first cholinesterase inhibitor approved for AD treatment, did not stop the progression of AD, producing only some cognitive improvements, but exhibited secondary effects mainly due to its hepatotoxicity. Thus, the drug was withdrawn from the clinics administration. Since then, many publications have described non‐hepatotoxic tacrines, and in addition, important efforts have been made to design multitarget tacrines by combining their cholinesterase inhibition profile with the modulation of other biological targets involved in AD. 相似文献
2.
Najahi E Sudor J Chabchoub F Nepveu F Zribi F Duval R 《Molecules (Basel, Switzerland)》2010,15(12):8841-8855
In this paper we present the room temperature synthesis of a novel serie of 1,4-disubstituted-1,2,3-triazoles 4a-l by employing the (3+2) cycloaddition reaction of pyrimidinones containing alkyne functions with different model azides in the presence of copper sulphate and sodium ascorbate. To obtain the final triazoles, we also synthesized the major precursors 6-amino-5-cyano-1,4-disubstituted-2(1H)-pyrimidinones 3a-r from ethyl 2,2-dicyanovinylcarbamate derivatives 2a-c and various primary aromatic amines containing an alkyne group. The triazoles were prepared in good to very good yields. 相似文献
3.
We reinvestigate the sign problem in the two-dimensional Hubbard model using the projector ground state Quantum Monte Carlo scheme with Langevin dynamics. Our interest is mainly motivated by the question: what is the parameter space in which simulations may be performed with reliable results and how does the average sign scales with inverse temperature? In the parameter space in which one may omit the sign problem we have studied the ground state properties: momentum distribution and spin structure. We find an exponential decay of the average sign. At half filling, we find evidence for an antiferromagnetic insulating ground state. At off half band fillings, the antiferromagnetic state is destroyed leaving place to an incommensurate spin density state. 相似文献
4.
Kamoun F Fguira IB Hassen NB Mejdoub H Lereclus D Jaoua S 《Applied biochemistry and biotechnology》2011,165(1):300-314
This study reports on the identification, characterization and purification of a new bacteriocin, named Bacthuricin F103,
from a Bacillus thuringiensis strain BUPM103. Bacthuricin F103 production began in the early exponential phase and reached a maximum in the middle of the
same phase. Two chromatographic methods based on high performance liquid chromatography and fast protein liquid chromatography
systems were used to purify Bacthuricin F103. Sodium dodecyl sulphate-polyacrylamide gel electrophoresis revealed that this
bacteriocin had a molecular weight of approximately 11 kDa. It also showed a wide range of thermostability of up to 80 °C
for 60 min and a broad spectrum of antimicrobial activity over a pH range of 3.0–10.0. This bacteriocin was noted, and for
the first time, to exhibit potent antimicrobial activity against Agrobacterium subsp. strains, the major causal agents of crown gall disease in tomato and vineyard crops, and against several challenging
organisms in food, such as Listeria monocytogenes and Bacillus cereus. Complete killing with immediate impact on cells was observed within a short period of time. The sequence obtained for Bacthuricin
F103 by direct N-terminal sequencing shared considerable homology with hemolysin. Bacthuricin F103 was noted to act through
the depletion of intracellular ions, which suggest that the cell membrane was a possible target to Bacthuricin F103. 相似文献
5.
Hybrid metaheuristics for the profitable arc tour problem 总被引:1,自引:0,他引:1
The profitable arc tour problem is a variant in the vehicle routing problems. It is included in the family of the vehicle routing with profit problems in which a set of vehicle tours are constructed. The objective is to find a set of cycles in the vehicle tours that maximize the collection of profits minus travel costs, subject to constraints limiting the length of cycles that profit is available on arcs. To solve this variant we adopted two metaheuristics based on adaptive memory. We show that our algorithms provide good results in terms of solution quality and running times. 相似文献
6.
A numerical study of the three-dimensional fluid flow has been carried out to determine the effects of the transverse aspect ratio, Ay, on the flow structure in two-sided non-facing lid-driven cavities. The flow is complex, unstable and can undergo bifurcation. The numerical method is based on the finite volume method and multigrid acceleration. Computations have been investigated for several Reynolds numbers and various aspect ratio values. At a fixed Reynolds number, Re=500, the three-dimensional flow characteristics are analyzed considering four transverse aspect ratios, Ay=1,0.75,0.5 and 0.25. It is observed that the transition to the unsteady regime follows the classical scheme of a Hopf bifurcation. An analysis of the flow evolution shows that, at Ay=0.75, the flow bifurcates to a periodic regime at (Re=600) with a frequency f=0.093 less than the predicted value in the cubical cavity. A correlation is established when Ay=0.5 and gives the critical Reynolds number value. At Ay=0.25, the periodic regime occurs at high Re value beyond 3500, after which the flow becomes chaotic. It is shown that, when increasing Ay over the unit, the flow in the cavity exhibits a complex behavior. The kinetic energy transmission from the driven walls to the cavity center is reduced at low Ay values. 相似文献
7.
Noura Beji Bassem Jarboui Mansour Eddaly Habib Chabchoub 《Journal of computational science》2010,1(3):159-167
The Redundancy Allocation Problem generally involves the selection of components with multiple choices and redundancy levels that produce maximum system reliability given various system level constraints as cost and weight. In this paper we investigate the series–parallel redundant reliability problems, when a mixing of components was considered. In this type of problem both the number of redundancy components and the corresponding component reliability in each subsystem are to be decided simultaneously so as to maximise the reliability of system. A hybrid algorithm is based on particle swarm optimization and local search algorithm. In addition, we propose an adaptive penalty function which encourages our algorithm to explore within the feasible region and near feasible region, and discourage search beyond that threshold. The effectiveness of our proposed hybrid PSO algorithm is proved on numerous variations of three different problems and compared to Tabu Search and Multiple Weighted Objectives solutions. 相似文献
8.
Oussama Graja Bacem Zghal Kajetan Dziedziech Fakher Chaari Adam Jablonski Tomasz Barszcz Mohamed Haddar 《Comptes Rendus Mecanique》2019,347(1):49-61
Planetary gearboxes are widely used in industrial machines. They usually work in harsh environments giving rise to damages and high maintenance costs. Condition monitoring is a key action allowing one to detect the presence of such damage ensuring healthy running conditions. The knowledge of the dynamic behavior of such a gearbox can be achieved using modeling tools as a primary step before conditioning the monitoring subject. In addition, modeling a gear set can help in the stage of design in order to optimize physical and geometric parameters of the system. Therefore, in this work, a two-dimensional lumped parameter model is adopted to build all vibration sources. The time-varying mesh stiffness is approximated as a square wave form. A novel mathematical formulation is proposed to model the amplitude modulation phenomenon due to the rotational motion of the planets around the center of the gearbox. Finally, the overall vibration signal is concluded as a summation of all vibration components influenced by the modulation function. 相似文献
9.
We describe here a rapid process for the preparation of new 9-chloromethyl-12-aryl-10,12-dihydrobenzo[5,6]chromeno[2,3-d]pyrimidin-11-ones 5a-d and 10-chloromethyl-7-aryl-7,9-dihydrobenzo[7,8]chromeno[2,3-d]pyrimidin-8-ones 6a-d by two different methods utilizing microwave irradiation. This methodology provides better yields(72%–80%) and high purity of the title compounds. 相似文献
10.
Ben Rebah F Smaoui S Frikha F Gargouri Y Miled N 《Applied biochemistry and biotechnology》2008,151(1):71-79
The lipase inhibitory activity of ethanol extracts obtained from some marine algae collected on the Tunisian coast was evaluated.
Caulerpa prolifera extract markedly reduced both dog gastric (DGL) and human pancreatic lipase (HPL) activities. Generally, the inhibition reached
100% after 40 to 60 min of incubation depending on lipase types and on substrates used. Moreover, the inhibitory effect of
C. prolifera extract on lipases appeared to be accelerated by adding bile salts, which likely modified the interface and allowed the inhibitory
compound to inactivate the lipase. The separation of C. prolifera extract by thin-layer chromatography (TLC) resulted in eight fractions showing efficient inhibition rate against DGL, compared
to the crude extract. In the case of HPL, TLC fractionation reduced the inhibitory rates, suggesting that the effect of algal
extract on lipases may be caused by a synergetic action of several compounds within the extract. High-performance liquid chromatograph
separation resulted in isolation of a major compound displaying high inhibition capacity of HPL activity. Caulerpa prolifera extract may therefore be useful in developing antiobesity drugs. 相似文献