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1.
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   
2.
The main objective of this paper is to demonstrate how greenhouse gas (GHG) emissions can be quantified during the evaluation of control strategies in wastewater treatment plants (WWTP). A modified version of the IWA Benchmark Simulation Model No 2 (BSM2G) is hereby used as a simulation case study. Thus, the traditional effluent quality index (EQI), operational cost index (OCI) and time in violation (TIV) used to evaluate control strategies in WWTP are complemented with a new dimension dealing with GHG emissions. The proposed approach is based on a set of comprehensive models that estimate all potential on-site and off-site sources of GHG emissions. The case study investigates the overall performance of several control strategies and demonstrates that substantial reductions in effluent pollution, operating costs and GHG emissions can be achieved when automatic control is implemented. Furthermore, the study is complemented with a scenario analysis that examines the role of i) the dissolved oxygen (DO) set-point, ii) the sludge retention time (SRT) and iii) the organic carbon/nitrogen ratio (COD/N) as promoters of GHG emissions. The results of this study show the potential mechanisms that promote the formation of CO2, CH4 and N2O when different operational strategies are implemented, the existing synergies and trade-offs amongst the EQI, the OCI and TIV criteria and finally the need to reach a compromise solution to achieve an optimal plant performance.  相似文献   
3.
AC traction systems are 1 × 25 or 2 × 25 kV 50-Hz single-phase, non-linear, time-varying loads that can cause power quality problems. One of the main concerns about these systems is voltage distortion, because adjustable-speed drives for trains may inject harmonic currents of frequencies below 2 kHz. Since the presence of parallel resonances in the contact feeder section of the traction circuit worsens the scenario, traction system resonance phenomena should be analyzed to prevent problems. Several works addressed these phenomena, but they only drew weak numerical conclusions based on the frequency scan method. This article studies 1 × 25 kV traction system resonances at pantograph terminals and provides more effective analytical expressions to locate them and determine the impact of traction system parameters on them. These expressions are validated from several traction systems in the literature.  相似文献   
4.
Self-propelled micromotors are emerging as important tools that help us understand the fundamentals of motion at the microscale and the nanoscale. Development of the motors for various biomedical and environmental applications is being pursued. Multiple fabrication methods can be used to construct the geometries of different sizes of motors. Here, we present an overview of appropriate methods of fabrication according to both size and shape requirements and the concept of guiding the catalytic motors within the confines of wall. Micromotors have also been incorporated with biological systems for a new type of fabrication method for bioinspired hybrid motors using three-dimensional (3D) printing technology. The 3D printed hybrid and bioinspired motors can be propelled by using ultrasound or live cells, offering a more biocompatible approach when compared to traditional catalytic motors.  相似文献   
5.
We report on the fabrication of polyelectrolyte multilayer-coated hollow silicon dioxide micropillars as pH-responsive drug delivery systems. Silicon dioxide micropillars are based on macroporous silicon formed by electrochemical etching. Due to their hollow core capable of being loaded with chemically active agents, silicon dioxide micropillars provide additional function such as drug delivery system. The polyelectrolyte multilayer was assembled by the layer-by-layer technique based on the alternative deposition of cationic and anionic polyelectrolytes. The polyelectrolyte pair poly(allylamine hydrochloride) and sodium poly(styrene sulfonate) exhibited pH-responsive properties for the loading and release of a positively charged drug doxorubicin. The drug release rate was observed to be higher at pH 5.2 compared to that at pH 7.4. Furthermore, we assessed the effect of the number of polyelectrolyte bilayers on the drug release loading and release rate. Thus, this hybrid composite could be potentially applicable as a pH-controlled system for localized drug release.  相似文献   
6.
Automatic segmentation of multiple sclerosis (MS) lesions in brain MRI has been widely investigated in recent years with the goal of helping MS diagnosis and patient follow-up. However, the performance of most of the algorithms still falls far below expert expectations. In this paper, we review the main approaches to automated MS lesion segmentation. The main features of the segmentation algorithms are analysed and the most recent important techniques are classified into different strategies according to their main principle, pointing out their strengths and weaknesses and suggesting new research directions. A qualitative and quantitative comparison of the results of the approaches analysed is also presented. Finally, possible future approaches to MS lesion segmentation are discussed.  相似文献   
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8.
‘Real-Time’ is one of the most frequent concepts used referring to digital media. Despite it is commonly related to immediate feedback, it is not clear when it happens and what its characteristics are, especially in current digital interfaces. Although real-time has been written about very extensively in the context of Human Computer Interaction and Computational Systems, there are few studies evaluating the key features of real-time interaction in other domains. This article attempts to address this situation by proposing a new approach to the concept of real-time interaction driving the analysis of this topic into paradigmatic cases studies in new media, video games and digital artworks. This new analysis reveals several specific facets that allow us to identify new factors in the understanding of this fuzzy concept. Finally, the article proposes a new definition of ‘real-time interaction’ based on the findings in the context of new media practices.  相似文献   
9.
There is a distribution limit of sessile oak (Quercus petraea) in the northern half of the Iberian Peninsula, with its southernmost populations located at the xeric limit for the species. We present here the current distribution of these populations in the Montseny Massif (N.E. Catalonia) and how the surface area they cover has developed over the last 50 years. Using a new high-resolution map (1:5000) we have calculated that Q. petraea currently covers 64.1 ha, and is found between 450 and 1150 m above sea level with a predominantly southern exposure, with the north-facing slopes being dominated by beech forests. With regard to its recent development, 44% of what is now dense forest was, in 1956, much more dispersed while 11% of it consisted of open spaces or shrubs. Such changes clearly show that, in Montseny, Q. petraea is well capable of regenerating its forest canopy as well as colonising adjacent environments.  相似文献   
10.
Designing coordinated robot behaviors in uncertain, dynamic, real-time, adversarial environments, such as in robot soccer, is very challenging. In this work we present a case-based reasoning approach for cooperative action selection, which relies on the storage, retrieval, and adaptation of example cases. We focus on cases of coordinated attacking passes between robots in the presence of the defending opponent robots. We present the case representation explicitly distinguishing between controllable and uncontrollable indexing features, corresponding to the positions of the team members and opponent robots, respectively. We use the symmetric properties of the domain to automatically augment the case library. We introduce a retrieval technique that weights the similarity of a situation in terms of the continuous ball positional features, the uncontrollable features, and the cost of moving the robots from the current situation to match the case controllable features. The case adaptation includes a best match between the positions of the robots in the past case and in the new situation. The robots are assigned an adapted position to which they move to maximize the match to the retrieved case. Case retrieval and reuse are achieved within the distributed team of robots through communication and sharing of own internal states and actions. We evaluate our approach, both in simulation and with real robots, in laboratory scenarios with two attacking robots versus two defending robots as well as versus a defender and a goalie. We show that we achieve the desired coordinated passing behavior, and also outperform a reactive action selection approach.  相似文献   
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