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See detailDesign, synthesis and pharmacological evaluation of sulfonylureas and sulfonycyanoguanidines as thromboxane A2 receptor antagonists. Insights into selectivity between thromboxane A2 receptor isoforms (TPα et TPβ)
Hanson, Julien ULg

Doctoral thesis (2007)

Thromboxane A2 (TXA2) is an important mediator metabolized from arachidonic acid through the cyclooxygenase pathway, mainly in platelets and macrophages. It is a potent inducer of platelet aggregation and ... [more ▼]

Thromboxane A2 (TXA2) is an important mediator metabolized from arachidonic acid through the cyclooxygenase pathway, mainly in platelets and macrophages. It is a potent inducer of platelet aggregation and smooth muscle contraction. Its overproduction has been detected in pathologies such as stroke, asthma, myocardial infarction or atherosclerosis. The action of TXA2 is mediated by a specific G-protein coupled receptor (TP) of which two alternative spliced isoforms, TPalpha and TPbeta, have been described. The exact role of these two isoforms is not clearly understood. However, recent studies have described their implications in vascular physiology and pathology. The inhibition of the action of TXA2 on platelets and blood vessels would be interesting as original therapies against cardiovascular diseases. Consequently, the design of TP receptor antagonists remains of great interest in cardiovascular medicine. In the laboratory of medicinal chemistry (University of Liège, Belgium), several nitrobenzenesulfonylureas, derived from torasemide (a loop diuretic), have been previously described as TP receptor antagonists. Two compounds, BM573 and BM613 were among the most interesting molecules identified in that previous work. The present project is divided in two parts. First, we have determined the pharmacological properties of BM573 and BM613 as thromboxane synthase inhibitors and TP receptor antagonists, in vitro and in vivo. In our assays, these two compounds were proved to have high affinity for both TPalpha and TPbeta, to be potent antiplatelet agents, to inhibit thromboxane synthase and TP-mediated smooth muscle contraction. Additionally, they significantly reduced the size of the thrombus in a rat model of ferric chloride-induced arterial thrombosis. Consequently, we demonstrated that the TP receptor antagonists BM573 and BM613, belonging to the chemical family of nitrobenzenesulfonylureas, could be regarded as antiplatelet and antithrombotic agents potentially useful in thromboxane-related diseases such as stroke or myocardial infarction. Secondly, given the interesting pharmacological profile of BM573 and BM613, we have designed and synthesized several series of compounds derived from these two agents. We have evaluated the binding properties (affinity) of the first generation (+/- 35 original derivatives) of compounds on either TPalpha or TPbeta, transiently expressed in COS-7 cell lines. Additionally, we have measured the ability of our drugs to inhibit the intracellular calcium mobilization upon TPalpha or TPbeta stimulation. To confirm our results, we also assessed the antiplatelet properties of our drugs by means of determination of inhibition of human platelet aggregation. On the basis of the results obtained with these in vitro assays, we have synthesized and evaluated a second generation of derivatives (+/- 35 original compounds) and improved the selectivity of several original compounds for TP receptor isoforms. The originality of this work was to evaluate a large library of synthetic compounds on both TP receptor isoforms, using specific pharmacological tests. By means of structure-activity relationship studies, we were able to identify chemical groups implicated in selectivity and to propose lead compounds for development of highly specific TPalpha or TPbeta antagonists. Besides, we have identified an in vivo drug candidates for prevention of thrombosis and pathological platelet aggregation. [less ▲]

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See detailDesign, synthesis and pharmacology of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas
Masereel, B.; Ouedraogo, R.; Dogne, J.-M. et al

in Journal de Pharmacie de Belgique (1998), 53

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See detailDesign, synthesis and pharmacology of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas
Masereel, B.; Ouedraogo, R.; Dogne, J. M. et al

Poster (1997, May)

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See detailDesign, synthesis, and pharmacological evaluation of cromakalim analogues as pancreatic β-cell-selective KATP channel openers
Florence, X.; De Tullio, Pascal ULg; Lebrun, Ph. et al

Conference (2007, October)

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See detailDesign, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors
Francotte, Pierre ULg; De Tullio, Pascal ULg; Goffin, Eric ULg et al

in Journal of Medicinal Chemistry (2007), 50(13), 3153-3157

A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the ... [more ▼]

A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the 7-position of the heterocycle. The biological evaluation was achieved by measuring the AMPA current in rat cortex mRNA-injected Xenopus oocytes. The most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (12a) was found to be active in an object recognition test in rats demonstrating cognition enhancing effects in vivo after oral administration. [less ▲]

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See detailLes désignations de plats étrangères dans le Cuisnier gascon (1740)
Colson, Maryse ULg

Conference (2011, May 13)

Œuvre originale de la première moitié du XVIIIe siècle, Le Cuisinier gascon est certainement l’un des ouvrages culinaires les plus énigmatiques de son époque. Publié de façon anonyme, le livre est ... [more ▼]

Œuvre originale de la première moitié du XVIIIe siècle, Le Cuisinier gascon est certainement l’un des ouvrages culinaires les plus énigmatiques de son époque. Publié de façon anonyme, le livre est aujourd’hui attribué au Prince de Dombes, frère du comte d’Eu et grand veneur de Louis XV avec lequel il partage le goût de la chasse et des bons repas. L’ouvrage présente deux cent dix-sept recettes disparates dont l’écriture ne déroge à aucune règle fondamentale : concision et efficacité du style, sobriété de la syntaxe, homogénéité des moyens d’expression de l’injonction. En effet, la recette de cuisine, par sa nature prescriptive, laisse peu de place aux figures stylistiques et à la créativité de son auteur. En réalité, le seul espace qui permet de laisser quelque latitude à l’imagination est concentré dans l’intitulé du plat décrit. Or, Le Cuisinier gascon présente de nombreuses désignations de plats fantaisistes et, en particulier, un nombre impressionnant de dénominations « étrangères » telles que les Cuisses de poularde à la Suisse ou les Poulpettes à l’Italienne. Il est donc évident que l’ouvrage se veut cosmopolite, résolument tourné vers l’ailleurs – qu’il soit géographique ou imaginaire. De manière générale, nous nous demanderons dans quelle mesure les emprunts lexicaux tels que Woatre fiche, oille et niocs peuvent être considérés comme des transferts culturels, à la fois matériel (la spécialité culinaire) et linguistique (sa dénomination). Peut-on voir dans cet exotisme culinaire le signe d’influences culturelles entre des pays dont les frontières politiques ne cessent de se redessiner durant un siècle éclairé par les Lumières ? En particulier, deux types de désignations problématiques retiendront notre attention ; le premier type portant sur « l’ailleurs spatial » et le second sur « l’ailleurs imaginaire ». Premièrement, on note de nombreux adjectifs invariables construits sur le modèle « à la + adj. fém. sg. » : les uns réfèrent à des régions (à la Provençale) et les autres à des entités culturelles plus vastes (à l’Espagnole). Si le lien entre la désignation et la référence est parfois évident (par exemple, on trouve presque invariablement du parmesan dans la composition des plats à l’Italienne), il peut s’avérer abscons dans d’autres cas ; ainsi, nous rencontrons des Choux à la Turque et des Foyes gras à l’Indienne qui n’ont rien d’oriental. Ces qualifications sont-elles purement fantaisistes ou ont-elles une explication rationnelle ? Ces adjectifs font-il véritablement référence à une nation ou plutôt à une tradition, à un événement historique ou à une personnalité ? Deuxièmement, on observe des désignations inédites, propres au Cuisinier gascon : les Yeux de veau farcis au gratin, le Hachis d’œufs sans malice et le Veau en crotte d’âne roulé à la Nenteau en sont les meilleurs exemples. Ici, ce ne sont plus les frontières géographiques qui sont franchies, mais celles du réel. Comment comprendre l’étrangeté de ces appellations qui mêlent la représentation imagée des aliments et une poésie pleine d’humour ? Ne pourrait-on lire dans cette liberté nominative la volonté de l’auteur-cuisinier de s’émanciper en s’appropriant la matière culinaire grâce à l’usage qu’il fait de la langue ? Par l’étude de quelques désignations, nous verrons à quel point les transferts culturels imprègnent la gastronomie de l’époque et lui permettent d’évoluer. De plus, nous envisagerons la possibilité que le cuisinier, en introduisant l’étrange ou l’étranger dans son texte, devienne lui-même autre (un véritable auteur) et qu’il emmène le genre culinaire vers un ailleurs: la gasconnade. [less ▲]

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See detailLes désignations romanes de l'ECUREUIL
Boutier, Marie-Guy ULg; Baiwir, Esther ULg

in Contini, Michel; Veny, Joan (Eds.) Atlas linguistique roman (ALiR) (in press)

L'ALiR a pour objectif de fournir une description globale du lexique roman par champ sémantique, à travers l'étude onomasiologique des désignations romanes de concepts. Les analyses lexicale, phonétique ... [more ▼]

L'ALiR a pour objectif de fournir une description globale du lexique roman par champ sémantique, à travers l'étude onomasiologique des désignations romanes de concepts. Les analyses lexicale, phonétique, morphosyntaxiques sont mises en valeur par la production de cartes interprétatives. [less ▲]

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See detailDesigned combination of chiral selectors for adjustment of enantioseparation selectivity in capillary electrophoresis.
Fillet, Marianne ULg; Chankvetadze, Bezhan; Crommen, Jacques ULg et al

in Electrophoresis (1999), 20(13), 2691-7

In this study an attempt has been made to explain the reasons for changing the enantioseparation selectivity in some dual cyclodextrin (CD) systems compared to the use of single chiral selectors in ... [more ▼]

In this study an attempt has been made to explain the reasons for changing the enantioseparation selectivity in some dual cyclodextrin (CD) systems compared to the use of single chiral selectors in capillary electrophoresis (CE). An explanation for selectivity changes is proposed based on the effect of the chiral selector on the mobility of the analyte. In order to support the proposed mechanism, several dual systems were designed on the basis of the known recognition pattern of enantiomers for individual CDs. In most cases the separation selectivity could be adjusted in a designed way. There was no experimental evidence for simultaneous binding of a given chiral analyte with both chiral selectors or of chiral recognition of an analyte complex with one CD by another CD. [less ▲]

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See detailDesigners Guide to EN 1998-1 and 1998-5. Eurocode 8: Design Provisions for Earthquake Resistant Structures
Carvalho; Elnashai; Fardis et al

in Designers Guide to EN 1998-1 and 1998-5. Eurocode 8: Design Provisions for Earthquake Resistant Structures (2005)

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See detailDesigning a linear pension scheme with forced savings and wage heterogeneity
Cremer, Helmuth; De Donder, Philippe; Maldonado, Dario et al

in International Tax and Public Finance (2007)

This paper studies the optimal linear pension scheme when society consists of rational and myopic individuals. Myopic individuals have, ex ante, a strong preference for the present even though, ex post ... [more ▼]

This paper studies the optimal linear pension scheme when society consists of rational and myopic individuals. Myopic individuals have, ex ante, a strong preference for the present even though, ex post, they would regret not to have saved enough. While rational and myopic persons share the same ex post intertemporal preferences, only the rational agents make their savings and labor supply decisions according to these preferences. Individuals are also distinguished by their productivity. The social objective is “paternalistic”: the utilitarian welfare function depends on ex post utilities. We examine how the presence of myopic individuals affects both the size of the pension system and the degree of redistribution it operates, with and without liquidity constraints. The relationship between proportion of myopic individuals and characteristics of the pension system turns out to be much more complex than one would have conjectured. Neither the impact on the level of pensions nor the effect on their redistributive degree is unambiguous. Nevertheless, we show that under some plausible assumptions adding myopic individuals increases the level of pension benefits and leads to a shift from a flat or even targeted scheme to a partially contributory one. However, we also provide an example where the degree of redistribution is not a monotonic function of the proportion of myopic individuals. [less ▲]

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See detailDesigning a new scaffold for Anterior Cruciate Ligament tissue engineering
Laurent, Cédric ULg

in Computer Methods in Biomechanics & Biomedical Engineering (2010)

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See detailDesigning a Platform for Flexible and Performant Virtual Routers on Commodity Hardware
Egi, Norbert; Greenhalgh, Adam; Handley, Mark et al

in Electronic Communications of the EASST (2009)

Multi-core CPUs, along with recent advances in memory and buses, render commodity hardware a strong candidate for software router virtualization. In this context, we present the design of a new platform ... [more ▼]

Multi-core CPUs, along with recent advances in memory and buses, render commodity hardware a strong candidate for software router virtualization. In this context, we present the design of a new platform for virtual routers on x86 hardware. We also elaborate on our design choices in order to achieve both high performance and flexibility for packet processing. [less ▲]

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See detailDesigning and implementing a GIS in an international context
Pantazis, Dimos N; Cornélis, Bernard ULg

in Transactions in GIS (1997), 1(4), 301-320

International collaborations between private companies, national research laboratories, and universities in the field of GIS have opened up new ways of exchanging knowledge and experiences between ... [more ▼]

International collaborations between private companies, national research laboratories, and universities in the field of GIS have opened up new ways of exchanging knowledge and experiences between different countries. However, when a collaboration involves the actual design and implementation of an operational GIS, rather than simply theoretical or applied research, or the development of specific applications, many problems can arise, sometimes leading either to the partial success or the complete failure of the project. Some of these problems are frequently encountered in all kinds of international collaborations: problems arising from different cultural mentalities, difficulties establishing a single common leadership, difficulties with communication and information exchange, and so on. Problems relating to the specific nature of the GIS are also present, for example the absence of digital geographic data format standards, the absence of metadata standards, the omission to use GIS or IS design methods, etc. This paper focuses on a joint Sino-Belgian project for the design and implementation of an urban geographical information system (UGIS) integrating remote sensing techniques in Hangzhou city, China and examines the general, specific, and international aspects of the problems encountered in an international collaboration. [less ▲]

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See detailDesigning and testing an air-PCM heat exchanger for building ventilation application coupled to energy storage
Dechesne, Bertrand ULg; Gendebien, Samuel ULg; Martens, Jonathan et al

in 2014 Purdue Conferences Proceedings (2014)

This paper studies a PCM heat exchanger coupled to a building ventilation system. This PCM module can either store heat during the day (e.g. by cooling solar PV panels) and restore it to the building ... [more ▼]

This paper studies a PCM heat exchanger coupled to a building ventilation system. This PCM module can either store heat during the day (e.g. by cooling solar PV panels) and restore it to the building during the night for space heating purposes or store coolness during the night and give it back during the day and thus act as a free cooling system. This project aims to develop a performing air-PCM heat exchanger providing latent energy storage of 0.5 kWh, this energy is delivered between 15 and 30°C. This heat exchanger is based on corrugated cells that can be easily filled, lined up and then locked in a box, letting the air pass between the cells. The PCM used for the prototype is c omposed of fatty acids. In order to develop an efficient PCM ventilation module, two different ways of investigation were followed and used in parallel. The first one used CFD simulations and the second one, a semi-empirical model based on correlations. The CFD simulations were able to predict the convection coefficient on the air side and also show the flow repartition between the different channels whereas the semi-empirical model allowed a parametrical study in order to identify the best geometry possible. Once the heat exchanger geometry was optimized, a test bench was built and a prototype of air-PCM heat exchanger was manufactured in order to measure its thermal and hydraulic performances. The tests consist in either a complete solidification or liquefaction of the PCM starting from respectively liquid PCM at 30°C or solid PCM at 15°C. The airflow rate was set to 45m³/h, which corresponds barely to the ventilation rate of a traditional room in a residential building. A comparison between the models and the measurements was carried out in order to calibrate the semi-empirical model. It will be shown that a simple semi-empirical model satisfactorily predicts the evolution of heat transfer rate for different operating conditions. [less ▲]

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See detailDesigning Courses on the Nature and History of Science
Leyh, Bernard ULg; Avitabile, Gustavo; Kelly, Orla

in Maciejowska, Iwona; Byers, Bill (Eds.) A Guidebook of Good Practice for the Pre-Service Training of Chemistry Teachers (2015)

Achieving scientific literacy is recognized as an essential goal of secondary school education. This obviously implies that science teachers, themselves, need to be scientifically literate, which in turn ... [more ▼]

Achieving scientific literacy is recognized as an essential goal of secondary school education. This obviously implies that science teachers, themselves, need to be scientifically literate, which in turn requires that emphasis should be placed on Nature of Science (NoS) issues in university pre-service (and also in-service) teacher education courses. A review of the research literature reveals that the beliefs and the understanding of teachers about NoS are often simplistic and lacking internal consistency. Research has also shown that explicit approaches towards NoS teaching are more efficient than implicit ones, and that analysis of historic cases can be an effective teaching tool. Based on an analysis of the existing literature and on their teaching experience, the authors propose a NoS curriculum for pre-service science teachers in chemistry, biology and physics and critically discuss a case example of NoS teaching practice consisting of four weekly seminars of two hours each. These seminars focus on identifying the learners’ preconceptions through team work, on discussing explicitly key NoS concepts and epistemological theories based on an inductive approach, and on highlighting the pedagogical implications. Suggestions for teaching the history of science (with emphasis on chemistry) are also provided. [less ▲]

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See detailDesigning large-scale CO2 capture units with assessment of solvent degradation
Léonard, Grégoire ULg; Crosset, Cyril; Dumont, Marie-Noëlle ULg et al

Poster (2014, October)

Solvent degradation is a major drawback for the large-scale implementation of post-combustion CO2 capture due to amine consumption and emission of degradation products. In the present work, we refine a ... [more ▼]

Solvent degradation is a major drawback for the large-scale implementation of post-combustion CO2 capture due to amine consumption and emission of degradation products. In the present work, we refine a previous kinetic model for describing solvent oxidative and thermal degradation based on experimental results. The CO2 capture process is then modeled in Aspen Plus with assessment of solvent degradation. As a result, this work provides a useful tool for the identification of optimal operating conditions that minimize both the energy and environmental impacts of the process. [less ▲]

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