Advances in prodrug design

The background of prodrug design is presented herein as the basis for introducing new and advanced latent systems, taking into account mainly the versatility of polymers and other macromolecules as carriers. PDEPT (Polymer-Directed Enzyme Prodrug Therapy); PELT (Polymer-Enzyme Liposome Therapy); CDS (Chemical Delivery System); ADEPT(Antibody-Directed Enzyme Prodrug Therapy); GDEPT/VDEPT (Gene-Directed Enzyme Prodrug Therapy/Virus-Directed Enzyme Prodrug Therapy); ODDS (Osteotropic Drug Delivery System) and LEAPT (Lectin-directed enzyme-activated prodrug therapy) are briefly described and some examples are given. © 2005 Bentham Science Publishers Ltd.

Molecular hybridization: A useful tool in the design of new drug prototypes

Molecular hybridization is a new concept in drug design and development based on the combination of pharmacophoric moieties of different bioactive substances to produce a new hyrid compound with improved affinity and efficacy, when compared to the parent drugs. Additionally, this strategy can results in compounds presenting modified selectivity profile, different and/or dual modes of action and reduced undesired side effects. So, in this described several example of different strategies for drug design, discovery and pharmacomodulation focused on new innovative hybrid compounds presenting analgesic, anti-inflammatory, platelet anti-aggregating, anti-infections, anticancer, cardio- and neuroactive properties.

Orientation, building height and sky view factor as energy efficiency design parameters

The energy efficiency of buildings should be a goal at the pre-design phase, though the importance of the design variables is often neglected even during the design process. Highlighting the relevance of these design variables, this research studies the relationships of building location variables with the electrical energy consumption of residential units. The following building design parameters are considered: orientation, story height and sky view factor (SVF). The consideration of the SVF as a location variable contributes to the originality of this research. Data of electrical energy consumption and users' profiles were collected and several variables were considered for the development of an Artificial Neural Network model. This model allows the determination of the relative importance of each variable. The results show that the apartments' orientation is the most important design variable for the energy consumption, although the story height and the sky view factor play a fundamental role in that consumption too. We pointed out that building heights above twenty-four meters do not optimize the energy efficiency of the apartments and also that an increasing SVF can influence the energy consumption of an apartment according to their orientation.

A multiagent architecture for supervisory and control system

Supervising and controlling the many processes involved in petroleum production is both dangerous and complex. Herein, we propose a multiagent supervisory and control system for handle continuous processes like those in chemical and petroleum industries In its architeture, there are agents responsible for managing data production and analysis, and also the production equipments. Fuzzy controllers were used as control agents. The application of a fuzzy control system to managing an off-shore installation for petroleum production onto a submarine separation process is described. © 2008 IEEE.

Reforming the international financial architecture: consensus and divergence

Includes bibliography

International asymmetries and the design of the International Financial System

Includes bibliography

Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases

Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland.

Design of experimental composting of animal carcasses in universitary unit of treatment aimed a correct final disposition and soil improve

For many years, composting has been used as a result of the recycling of organic matter. There is significative animal carcasses accumulation from teaching and researching activities of the university veterinary hospital. Every year, Unesp University needs to dispose correctly about 180 tones of this waste and the composting seemed to be the most sustainable alternative. Piles of animal carcasses were prepared using peanut hulls and tree pruning as bulking agent and water to the first phase of this process. The extracts pH values no impediments for offering germination and indicated a good addition to the soil management. The germination index showed no impediment to the seeds germination on any type of compost and the extracts concentrations not influenced this biological process. No parameters studied assigns risks of contamination of carcasses for the compost development in Unesp according to the proposed design. © 2013 Taylor & Francis Group.

Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates

The present work reports on the synthesis, biological assaying and docking studies of a series of 12 aryl thiosemicarbazones, which were planned to act over two main enzymes, cruzain and trypanothione reductase. These enzymes are used as targets of trypanocidal activity in Chagas disease control with a minimal mutagenic profile. Three p-nitroaromatic thiosemicarbazones showed high activity against Trypanosoma cruzi in in vitro assays (IC50 < 57 μM), and no mutagenic profile was observed in micronucleous tests. Although the in vitro inhibition test showed that 10-μM doses of eight compounds inhibited cruzain activity, no correlation was found between cruzain inhibition and trypanocidal activity. © 2013 Elsevier Masson SAS. All rights reserved.

Design da notícia: o desenvolvimento da indústria gráfica e a comunicação visual no Jornal Diário

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Arte concreta: racionalismo e abstração como contribuições para o design - um estudo na obra de Geraldo de Barros

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

A influência do design na aplicação de forças manuais para abertura de embalagens plásticas de refrigerantes

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

GAIA - Uma proposta de agente inteligente acoplado a algoritmos evolucionários para ajuste dinâmico de parâmetros através de conceitos de design inteligente e lógica fuzzy

Há muitos anos, técnicas de Computação Evolucionária vem sendo aplicadas com sucesso na solução dos mais variados tipos de problemas de otimização. Na constante procura pelo ótimo global e por uma melhor exploração da superfície de busca, as escolhas para ajustar estes métodos podem ser exponencialmente complexas e requerem uma grande quantidade de intervenção humana. Estes modelos tradicionais darwinianos apóiam-se fortemente em aleatoriedade e escolhas heurísticas que se mantém fixas durante toda a execução, sem que acompanhem a variabilidade dos indivíduos e as eventuais mudanças necessárias. Dadas estas questões, o trabalho introduz a combinação de aspectos da Teoria do Design Inteligente a uma abordagem hibrida de algoritmo evolucionário, através da implementação de um agente inteligente o qual, utilizando lógica fuzzy, monitora e controla dinamicamente a população e seis parâmetros definidos de uma dada execução, ajustando-os para cada situação encontrada durante a busca. Na avaliação das proposições foi construído um protótipo sobre a implementação de um algoritmo genético para o problema do caixeiro viajante simétrico aplicado ao cenário de distância por estradas entre as capitais brasileiras, o que permitiu realizar 580 testes, simulações e comparações entre diferentes configurações apresentadas e resultados de outras técnicas. A intervenção inteligente entrega resultados que, com sucesso em muitos aspectos, superam as implementações tradicionais e abrem um vasto espaço para novas pesquisas e estudos nos aqui chamados: “Algoritmos Evolucionários Híbridos Auto-Adaptáveis”, ou mesmo, “Algoritmos Evolucionários Não-Darwinianos”.

Avaliação de força de preensão manual e teste de usabilidade em embalagens com tampas de segurança: parâmetros para o design ergonômico

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Design sistêmico e ecoinovação em APLs: o método F.L.O.R.A como estratégia sustentável aplicada para o polo de confecções de Pernambuco

Pós-graduação em Design - FAAC