Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: Discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole

In this work we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and platelet anti-aggregating properties of new 3-(arylideneamino)-2-methyl-6,7-methylenedioxy-quinazolin-4 (3H)-one derivatives (3a-j), designed as conformationally constrained analogues of analgesic 1,3- benzodioxolyl-N- acylhydrazones (1) previously developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (2) as starting material. The pharmacological assays lead us to identify compounds LASSBio-1240 (3b) and LASSBio-1272 (3d) as new analgesic prototypes, presenting an antinociceptive pro. le more potent and effective than dipyrone and indomethacin used, respectively, as standards in AcOH-induced abdominal constrictions assay and in the formalin test. These results confirmed the success in the exploitation of conformation restriction strategy for identification of novel cyclic N-acylhydrazone analogues with optimized analgesic profile (C) 2009 Elsevier Ltd. All rights reserved.

Outer Trust-Region Method for Constrained Optimization

Given an algorithm A for solving some mathematical problem based on the iterative solution of simpler subproblems, an outer trust-region (OTR) modification of A is the result of adding a trust-region constraint to each subproblem. The trust-region size is adaptively updated according to the behavior of crucial variables. The new subproblems should not be more complex than the original ones, and the convergence properties of the OTR algorithm should be the same as those of Algorithm A. In the present work, the OTR approach is exploited in connection with the ""greediness phenomenon"" of nonlinear programming. Convergence results for an OTR version of an augmented Lagrangian method for nonconvex constrained optimization are proved, and numerical experiments are presented.

"I'm not a box. There's more than four sides to me." : En kvalitativ textanalys av karaktären Kurt Hummel och den homosexuella stereotypen

Arbetet består av en närläsning av karaktären Kurt Hummel i tv-serien Glee med fokus på stereotyper för homosexuella män, och hur Kurt förhåller sig till dem stereotyperna. Studien är gjord utifrån ett queerteoretiskt perspektiv och visar att Kurt i viss mån framställs stereotypt i seriens tidigare avsnitt, men att han efter hand uppvisar ett djup och komplexitet som man inte ofta ser hos homosexuella karaktärer på tv.

Developing Box-Pushing Behaviours Using Evolutionary Robotics

The context of this report and the IRIDIA laboratory are described in the preface. Evolutionary Robotics and the box-pushing task are presented in the introduction.The building of a test system supporting Evolutionary Robotics experiments is then detailed. This system is made of a robot simulator and a Genetic Algorithm. It is used to explore the possibility of evolving box-pushing behaviours. The bootstrapping problem is explained, and a novel approach for dealing with it is proposed, with results presented.Finally, ideas for extending this approach are presented in the conclusion.

Minimization of stock weight during close-die forging of a spindle

In this paper, Finite Element method and full-scale experiments have been used to study a hot forging method for fabri-cation of a spindle using reduced initial stock size. The forging sequence is carried out in two stages. In the first stage, the hot rolled cylindrical billet is pre-formed and pierced in a closed die using a spherical nosed punch to within 20 mm of its base. This process of piercing or impact extrusion leads to high strains within the work piece but requires high press loads. In the second stage, the resulting cylinder is placed in a die with a flange chamber and upset forged to form a flange. The stock mass is optimized for complete die filling. Process parameters such as effective strain distribution, material flow and forging load in different stages of the process are analyzed. It is concluded from the simulations that minor modifications of piercing punch geometry to reduce contact between the punch and emerging vertical walls of the cylinder appreciably reduces the piercing load. In the flange chamber, a die surfaces angle of 52° instead of 45° is pro-posed to ensure effective material flow and exert sufficient tool pressure to achieve complete cavity filling. In order to achieve better compression, it is also proposed to shorten both the length of the inserted punch and the die “tongues” by a few mm.

Designens betydelse vid val av boxvin : En studie om konsumenters preferenser av designfaktorer på bag-in-box-vin.

På den svenska marknaden står bag-in-box-vin för över 50 procent av allt vin som säljs och Sverige är det land där bag-in-boxen fått starkast fäste i världen (Fremin, 2012). Det gör att bag-in-box-förpackningen är en stor och betydelsefull produkt för vintillverkare och att ha kunskap om säljande design är viktigt för grafiska formgivare samt övriga involverade företag. Den föreliggande studiens syfte var att undersöka vilka designfaktorer på bagin- box-förpackningar som påverkar konsumenternas val av vin i Sverige. Studien innefattade en visuell kartläggning som ämnade ge en överblick av utbudet på ett Systembolag. Detta genomfördes för att skapa en grund till den webbaserade enkätundersökningen som genomfördes under våren 2015. Resultaten visade att majoriteten av respondenterna valde vin baserat på förpackningens utseende och ansåg att de påverkades främst av färg, typsnitt, illustrationer och varumärken. Resultaten visade också att ju högre vinkunskap konsumenterna hade desto mindre påverkade designen deras val. Kvinnor och män hade generellt olika åsikter angående hur stor påverkan de olika designfaktorerna hade vid valet av bag-in-box-vin. Denna studie är endast ett avstamp till ett ämne som innefattar många påverkande faktorer. Det betyder att mer forskning krävs inom ämnet innan helt sanningsenliga resultat kan fastställas.

Understanding the "black box" of a health-promotion program : keys to enable health among older persons aging in the context of migration

Although the need to make health services more accessible to persons who have migrated has been identified, knowledge about health-promotion programs (HPPs) from the perspective of older persons born abroad is lacking. This study explores the design experiences and content implemented in an adapted version of a group-based HPP developed in a researcher-community partnership. Fourteen persons aged 70-83 years or older who had migrated to Sweden from Finland or the Balkan Peninsula were included. A grounded theory approach guided the data collection and analysis. The findings showed how participants and personnel jointly helped raise awareness. The participants experienced three key processes that could open doors to awareness: enabling community, providing opportunities to understand and be understood, and confirming human values and abilities. Depending on how the HPP content and design are being shaped by the group, the key processes could both inhibit or encourage opening doors to awareness. Therefore, this study provides key insights into how to enable health by deepening the understanding of how the exchange of health-promoting messages is experienced to be facilitated or hindered. This study adds to the scientific knowledge base of how the design and content of HPP may support and recognize the capabilities of persons aging in the context of migration.

Adaptive, Decentralized, And Real-Time Sampling Strategies For Resource Constrained Hydraulic And Hydrologic Sensor Networks

We discuss the development and performance of a low-power sensor node (hardware, software and algorithms) that autonomously controls the sampling interval of a suite of sensors based on local state estimates and future predictions of water flow. The problem is motivated by the need to accurately reconstruct abrupt state changes in urban watersheds and stormwater systems. Presently, the detection of these events is limited by the temporal resolution of sensor data. It is often infeasible, however, to increase measurement frequency due to energy and sampling constraints. This is particularly true for real-time water quality measurements, where sampling frequency is limited by reagent availability, sensor power consumption, and, in the case of automated samplers, the number of available sample containers. These constraints pose a significant barrier to the ubiquitous and cost effective instrumentation of large hydraulic and hydrologic systems. Each of our sensor nodes is equipped with a low-power microcontroller and a wireless module to take advantage of urban cellular coverage. The node persistently updates a local, embedded model of flow conditions while IP-connectivity permits each node to continually query public weather servers for hourly precipitation forecasts. The sampling frequency is then adjusted to increase the likelihood of capturing abrupt changes in a sensor signal, such as the rise in the hydrograph – an event that is often difficult to capture through traditional sampling techniques. Our architecture forms an embedded processing chain, leveraging local computational resources to assess uncertainty by analyzing data as it is collected. A network is presently being deployed in an urban watershed in Michigan and initial results indicate that the system accurately reconstructs signals of interest while significantly reducing energy consumption and the use of sampling resources. We also expand our analysis by discussing the role of this approach for the efficient real-time measurement of stormwater systems.

Tipificação molecular de amostras de Brucella spp. utilização a técnica de BOX-PCR

O gênero Brucella é formado por coco-bacilos Gram negativos patogênicos ao homem e animais, sendo classificado como patógeno de grupo de risco III. A identificação dessas bactérias apresenta várias limitações como: exigência de inoculação em vários meios, tempo de incubação longo e necessidade de soros imunes e bacteriófagos. Devido à sua alta patogenicidade e ao longo tempo de exposição dos laboratoristas à bactéria, a brucelose é uma das infecções mais freqüentemente adquiridas em laboratório. Além da contaminação em laboratório, a transmissão ao homem pode ocorrer através de animais infectados e ingestão de produtos derivados, como o leite cru. A procura de métodos rápidos de identificação das espécies e biovares pode ser útil para diminuir os riscos do manuseio desta bactéria e na tomada de medidas de controle epidemiológico. O principal objetivo deste trabalho foi facilitar a classificação de cepas de referência de Brucella spp. e isoladas no Brasil utilizando a técnica de rep-PCR com oligonucleotídeos do elemento BOX, uma seqüência repetida presente no genoma de várias bactérias. Foram analisados 38 isolados representando diferentes espécies e biovares de Brucella sp. e 13 isolados de gêneros relacionados como controle da especificidade da reação. Foi realizada uma confirmação prévia dos isolados de brucela por testes bioquímicos e PCR gênero-específica. A técnica de BOX-PCR agrupou todas as espécies e biovares de Brucella em um único grupo com nível de similaridade entre 100 e 74%. Diferenças entre os isolados, quanto a presença ou ausência de bandas, puderam ser observadas. Entretanto, essas divergências não caracterizam uma espécie ou biovar. Bandas comuns a todos os isolados de Brucella sp. podem caracterizar o gênero.

Operações booleanas entre objetos delimitados por surfels usando constrained BSP-trees

As áreas de visualização e modelagem baseados em pontos têm sido pesquisadas ativamente na computação gráfica. Pontos com atributos (por exemplo, normais) são geralmente chamados de surfels e existem vários algoritmos para a manipulação e visualização eficiente deles. Um ponto chave para a eficiência de muitos métodos é o uso de estruturas de particionamento do espaço. Geralmente octrees e KD-trees, por utilizarem cortes alinhados com os eixos são preferidas em vez das BSP-trees, mais genéricas. Neste trabalho, apresenta-se uma estrutura chamada Constrained BSP-tree (CBSP-tree), que pode ser vista como uma estrutura intermediárias entre KD-trees e BSP-trees. A CBSP-tree se caracteriza por permitir cortes arbitrários desde que seja satisfeito um critério de validade dos cortes. Esse critério pode ser redefinido de acordo com a aplicação. Isso permite uma aproximação melhor de regões curvas. Apresentam-se algoritmos para construir CBSP-trees, valendo-se da flexibilidade que a estrutura oferece, e para realizar operações booleanas usando uma nova classificação de interior/exterior.