32 resultados para 8-hydroxyquinolinate derivatives

em Instituto Politécnico do Porto, Portugal


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O trabalho descrito no presente documento reporta a preparação de derivados tetrapirrólicos iodados de tipo porfirina tornando-os potenciais veículos a meio de contraste iodado, usado em radiodiagnóstico. Com os resultados deste trabalho irá ser realizado um pedido de patente das moléculas e portanto, o acesso a este trabalho será restrito nos termos do Código da Propriedade Industrial, aprovado pelo Decreto de Lei nº 36/2003 de 5 de Março. Na primeira fase do trabalho, foi sintetizado o derivado porfirínico simétrico, meso-substituído, contendo um total de 8 iodos. Este foi preparado por condensação do pirrol e do aldeído iodado em meio ácido e na presença de nitrobenzeno. Foram ainda preparados as respetivas metaloporfirinas contendo os iões metálicos de manganês e gadolínio. Posteriormente foi avaliada a capacidade destes derivados atenuarem o feixe de raio-X, através da mediação das Unidades de Hounsfield, após serem adquiridas imagens por Tomografia Computorizada. Na segunda fase do trabalho procedeu-se ao estudo da influência destes compostos na diferenciação celular, usando como modelo as células de pré-adipócitos 3T3-L1. Foi avaliada a diferenciação celular, através da quantificação de lípidos das células maduras, marcados com Red Oil O, por espectrofotometria de Visível 3 e 10 dias após a administração dos derivados em estudo.

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O presente trabalho descreve o estudo da actividad e antimicrobiana de quarto derivados da quinoxalina N,N-dióxido: quinoxalina 1,4-dióxido, 2-metilquinoxalina 1,4- dióxido, 6-cloro-2,3-dimetilquinoxalina 1,4-dióxido e 3-benzoil-2-metilquinoxalina 1,4- dióxido contra as estirpes bacterianas Geobacillus stearothermophilus ATCC 10149, Escherichia coli ATCC 25922, Escherichia coli HB101, Escherichia coli (blaTEM, blaCTX-M) e Salmonella (blaCTX-M), assim como contra a estirpe de levedura Saccharomyces cerevisiae PYCC 4072. A determinação da concentração mínima inibitória (MIC) foi realizada pelo método de diluição. Os valores de MIC’s foram estimados para cada composto e estirpe. Os resultados obtidos sugerem potenciais novas drogas para quimioterapia.

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Although it is always weak between RFID Tag and Terminal in focus of the security, there are no security skills in RFID Tag. Recently there are a lot of studying in order to protect it, but because it has some physical limitation of RFID, that is it should be low electric power and high speed, it is impossible to protect with the skills. At present, the methods of RFID security are using a security server, a security policy and security. One of them the most famous skill is the security module, then they has an authentication skill and an encryption skill. In this paper, we designed and implemented after modification original SEED into 8 Round and 64 bits for Tag.

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Pneumocystis pneumonia (PCP) is one of the most frequent causes of mortality among HIV-infected patients. Primaquine (PQ) is an antimalarial 8-aminoquinoline effective against PCP when given in combination with clindamycin. This has drawn the attention of Medicinal Chemists towards the anti-PCP activity of 8-aminoquinolines, not only confined to those exhibiting antimalarial activity [1]. It is thought that anti-PCP 8-aminoquinolines exert their anti-PCP activity by acting on the electronic transport and redox system of the P. carinii pathogen [1]. Recently, our research group has been developing imidazolidin-4-one derivatives of PQ (Scheme 1), targeting novel compounds with improved therapeutic action, namely, higher resistance to metabolic inactivation, lower toxicity and equal or higher antimalarial activity than that of the parent drug [2,3]. These imidazolidin-4-ones were seen to block the transmission of rodent malaria, caused by Plasmodium berghei on BalbC mice, to the mosquito vector Anopheles stephensi [3]. The anti-PCP activity of our PQ derivatives is now under study and preliminary in vitro assays [4] show that some of the compounds exhibit slight to moderate activity after a 72 h incubation period against P. carinii. In one case, the IC50 was comparable to that of parent PQ. Both these studies and forthcoming results from ongoing biological assays will be presented and discussed.

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This paper discusses the fundamentals of negative probabilities and fractional calculus. The historical evolution and the main mathematical concepts are discussed, and several analogies between the two apparently unrelated topics are established. Based on the new conceptual perspective, some experiments are performed shading new light into possible future progress.

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Consider a single processor and a software system. The software system comprises components and interfaces where each component has an associated interface and each component comprises a set of constrained-deadline sporadic tasks. A scheduling algorithm (called global scheduler) determines at each instant which component is active. The active component uses another scheduling algorithm (called local scheduler) to determine which task is selected for execution on the processor. The interface of a component makes certain information about a component visible to other components; the interfaces of all components are used for schedulability analysis. We address the problem of generating an interface for a component based on the tasks inside the component. We desire to (i) incur only a small loss in schedulability analysis due to the interface and (ii) ensure that the amount of space (counted in bits) of the interface is small; this is because such an interface hides as much details of the component as possible. We present an algorithm for generating such an interface.

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This paper studies the optimization of complex-order algorithms for the discrete-time control of linear and nonlinear systems. The fundamentals of fractional systems and genetic algorithms are introduced. Based on these concepts, complexorder control schemes and their implementation are evaluated in the perspective of evolutionary optimization. The results demonstrate not only that complex-order derivatives constitute a valuable alternative for deriving control algorithms, but also the feasibility of the adopted optimization strategy.

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Compositional real-time scheduling clearly requires that ”normal” real-time scheduling challenges are addressed but challenges intrinsic to compositionality must be addressed as well, in particular: (i) how should interfaces be described? and (ii) how should numerical values be assigned to parameters constituting the interfaces? The real-time systems community has traditionally used narrow interfaces for describing a component (for example, a utilization/bandwidthlike metric and the distribution of this bandwidth in time). In this paper, we introduce the concept of competitive ratio of an interface and show that typical narrow interfaces cause poor performance for scheduling constrained-deadline sporadic tasks (competitive ratio is infinite). Therefore, we explore more expressive interfaces; in particular a class called medium-wide interfaces. For this class, we propose an interface type and show how the parameters of the interface should be selected. We also prove that this interface is 8-competitive.

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Optimization problems arise in science, engineering, economy, etc. and we need to find the best solutions for each reality. The methods used to solve these problems depend on several factors, including the amount and type of accessible information, the available algorithms for solving them, and, obviously, the intrinsic characteristics of the problem. There are many kinds of optimization problems and, consequently, many kinds of methods to solve them. When the involved functions are nonlinear and their derivatives are not known or are very difficult to calculate, these methods are more rare. These kinds of functions are frequently called black box functions. To solve such problems without constraints (unconstrained optimization), we can use direct search methods. These methods do not require any derivatives or approximations of them. But when the problem has constraints (nonlinear programming problems) and, additionally, the constraint functions are black box functions, it is much more difficult to find the most appropriate method. Penalty methods can then be used. They transform the original problem into a sequence of other problems, derived from the initial, all without constraints. Then this sequence of problems (without constraints) can be solved using the methods available for unconstrained optimization. In this chapter, we present a classification of some of the existing penalty methods and describe some of their assumptions and limitations. These methods allow the solving of optimization problems with continuous, discrete, and mixing constraints, without requiring continuity, differentiability, or convexity. Thus, penalty methods can be used as the first step in the resolution of constrained problems, by means of methods that typically are used by unconstrained problems. We also discuss a new class of penalty methods for nonlinear optimization, which adjust the penalty parameter dynamically.

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Nonlinear Optimization Problems are usual in many engineering fields. Due to its characteristics the objective function of some problems might not be differentiable or its derivatives have complex expressions. There are even cases where an analytical expression of the objective function might not be possible to determine either due to its complexity or its cost (monetary, computational, time, ...). In these cases Nonlinear Optimization methods must be used. An API, including several methods and algorithms to solve constrained and unconstrained optimization problems was implemented. This API can be accessed not only as traditionally, by installing it on the developer and/or user computer, but it can also be accessed remotely using Web Services. As long as there is a network connection to the server where the API is installed, applications always access to the latest API version. Also an Web-based application, using the proposed API, was developed. This application is to be used by users that do not want to integrate methods in applications, and simply want to have a tool to solve Nonlinear Optimization Problems.

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In Nonlinear Optimization Penalty and Barrier Methods are normally used to solve Constrained Problems. There are several Penalty/Barrier Methods and they are used in several areas from Engineering to Economy, through Biology, Chemistry, Physics among others. In these areas it often appears Optimization Problems in which the involved functions (objective and constraints) are non-smooth and/or their derivatives are not know. In this work some Penalty/Barrier functions are tested and compared, using in the internal process, Derivative-free, namely Direct Search, methods. This work is a part of a bigger project involving the development of an Application Programming Interface, that implements several Optimization Methods, to be used in applications that need to solve constrained and/or unconstrained Nonlinear Optimization Problems. Besides the use of it in applied mathematics research it is also to be used in engineering software packages.

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This paper proposes the calculation of fractional algorithms based on time-delay systems. The study starts by analyzing the memory properties of fractional operators and their relation with time delay. Based on the Fourier analysis an approximation of fractional derivatives through timedelayed samples is developed. Furthermore, the parameters of the proposed approximation are estimated by means of genetic algorithms. The results demonstrate the feasibility of the new perspective.

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In this paper a new method for the calculation of the fractional expressions in the presence of sensor redundancy and noise, is presented. An algorithm, taking advantage of the signal characteristics and the sensor redundancy, is tuned and optimized through genetic algorithms. The results demonstrate the good performance for different types of expressions and distinct levels of noise.

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Though the formal mathematical idea of introducing noninteger order derivatives can be traced from the 17th century in a letter by L’Hospital in which he asked Leibniz what the meaning of D n y if n = 1/2 would be in 1695 [1], it was better outlined only in the 19th century [2, 3, 4]. Due to the lack of clear physical interpretation their first applications in physics appeared only later, in the 20th century, in connection with visco-elastic phenomena [5, 6]. The topic later obtained quite general attention [7, 8, 9], and also found new applications in material science [10], analysis of earth-quake signals [11], control of robots [12], and in the description of diffusion [13], etc.