References of "Dupont, Léon"
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See detail8-Chloro-5-(4-methylpiperazin-1-yl)-11H-pyrido[2,3-b][1,5]benzoxazepine
Dupont, Léon ULg; Liégeois, Jean-François ULg

in Acta Crystallographica Section E-Structure Reports Online (2003), 59(Part 12), 1962-1963

The crystal structure of the title compound, C17H17ClN4O, has been undertaken as part of our studies of dopamine receptors. The oxazepine ring has a boat conformation, while the piperazine ring is in a ... [more ▼]

The crystal structure of the title compound, C17H17ClN4O, has been undertaken as part of our studies of dopamine receptors. The oxazepine ring has a boat conformation, while the piperazine ring is in a normal chair conformation. The dihedral angle between the two aromatic rings that lie on the same side of the oxazepine moiety is 113.99 (7)degrees. There is no hydrogen bonding. [less ▲]

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See detailUse of municipal solid waste incineration residues in the precasting of concrete paving
Courard, Luc ULg; Degeimbre, Robert ULg; Darimont, Anne ULg et al

in Materials and Structures (2002), 35(250), 365-372

Valorisation of Municipal Solid Waste Incineration Residues - excluding ashes - is a positive advance in sustainable development: saving natural resources, decrease in wastes volume stored, reduction of ... [more ▼]

Valorisation of Municipal Solid Waste Incineration Residues - excluding ashes - is a positive advance in sustainable development: saving natural resources, decrease in wastes volume stored, reduction of energy consumption. If good conditions of incineration can be ensured and post-combustion treatments are realised, solid residues are in the form of granular materials usable in construction and civil engineering. Uses in road structures are classical; application for the precasting of paving is quite new and interesting due to the quantity of recycled materials. Mechanical and physical performances of municipal solid waste incineration residues let us to replace a part of the granular skeleton and to obtain similar behaviour as with reference granular composition: splitting resistance, water absorption and resistance to abrasion are optimised. Leaching behaviour is also verified in order to avoid detrimental effect on the environment; it is shown that post-combustion treatments and compacting energy combined with vibration are essential for a good quality product fabrication. [less ▲]

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See detail8-Chloro-6-(3-dimethylaminopropylamino)-11H-pyrido[2,3-b][1,4]benzodiazepine
Dupont, Léon ULg; Eyrolles, Laurence; Evrard, Guy et al

in Acta Crystallographica Section E-Structure Reports Online (2002), 58(Part 1), 69-71

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well ... [more ▼]

The crystal structure determination of the title compound, C17H20ClN5, has been undertaken as part of studies on antipsychotic drugs. Its structure is compared with that of clozapine (C18H19ClN4), a well known atypical antipsychotic drug. The side chain is more flexible than in the N-methylpiperazine analogues, but its folding is influenced by an intramolecular N-H . . .N hydrogen bond. The distances between the N-distal atom, a possible pharmacophore, and the centres of the two aromatic rings are significantly shorter than in clozapine. The crystal packing involves one N-H . . .N intermolecular hydrogen bond. The title compound showed no affinity for the receptors tested. [less ▲]

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See detailNew 3-deoxyanthocyanidins from leaves of Arrabidaea chica
Devia, B.; Llabres, Gabriel ULg; Wouters, J. et al

in Phytochemical Analysis [=PCA] (2002), 13(2, Mar-Apr), 114-120

Two new 3-deoxyanthocyanidins, 6,7,3',4'-tetrahydroxy-5-methoxyflavylium and 6,7,4'-trihydroxy-5-methoxyflavylium, and the pigment carajurin, which has been previously identified, were isolated from dried ... [more ▼]

Two new 3-deoxyanthocyanidins, 6,7,3',4'-tetrahydroxy-5-methoxyflavylium and 6,7,4'-trihydroxy-5-methoxyflavylium, and the pigment carajurin, which has been previously identified, were isolated from dried leaves of Arrabidaea chica, a creeper native to the American tropics. The structures of the components were elucidated by H-1- and C-13-NMR spectroscopy and HPLC-MS, including X-ray crystallographic analysis for carajurin. Copyright (C) 2002 John Wiley Sons, Ltd. [less ▲]

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See detailLes activateurs de canaux potassiques: étude structurale comparative du pinacidil, du diazoxide et du cromakalim
Dupont, Léon ULg; Pirotte, Bernard ULg; De Tullio, Pascal ULg et al

in Annales Pharmaceutiques Françaises (1995), 53(5), 201-208

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers ... [more ▼]

A conformational analysis has been performed with SYBYL starting from the energy optimized (Tripos force field) X-ray conformation of (R,S)-pinacidil. The geometry of four selected low energy conformers has been reoptimized using the AM1 semiempirical Molecular Orbital method (MOPAC 5.0), and the total energy of the optimized conformers has been compared. In spite of an apparent structural dissimilarity, a good analogy has been found between the calculated isopotential map of diazoxide and that of at least one selected low energy conformer of pinacidil. It has been suggested that, unlike cromakalim, the low but observable activity of pinacidil on pancreatic B-cells could be explained by adoption for this compound of a conformation having a diazoxide-like stereoelectronical imprint which could assume a similar interaction on the same biological receptor. [less ▲]

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See detailModélisation moléculaire de l'usambarensine, de la tubulosine et de l'émétine, alcaloïdes cytotoxiques et antiamibiens
Quetin-Leclercq, J.; Dupont, Léon ULg; Wright, C. W. et al

in Journal de Pharmacie de Belgique (1991), 46(2, Mar-Apr), 85-92

The analyses of the different possible conformations of usambarensine, tubulosine and emetine, which possess interesting cytotoxic and amoebicide properties showed us that they cannot take the planar ... [more ▼]

The analyses of the different possible conformations of usambarensine, tubulosine and emetine, which possess interesting cytotoxic and amoebicide properties showed us that they cannot take the planar conformation proposed to explain the activity of this type of molecules on protein synthesis. Nevertheless, a common (non planar) conformation exists where the angles between the two plans containing the aromatic rings are nearly the same for the three compounds. This fact could confirm the hypothesis of a common receptor which would be slightly different in amoebae because of its higher sensitivity to usambarensine. [less ▲]

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See detailPaf-Receptor. 1. 'Cache-Oreilles' Effect of Selected High-Potency Platelet-Activating Factor (Paf) Antagonists
Dive, Georges ULg; Godfroid, Jean-Jacques; Lamotte-Brasseur, Josette et al

in Journal of Lipid Mediators (1989), 1(4, Jul-Aug), 201-15

Three-dimensional electrostatic maps were calculated for six potent antagonists of platelet-activating factor (PAF), the antagonists being selected for their apparent structural heterogeneity. The ... [more ▼]

Three-dimensional electrostatic maps were calculated for six potent antagonists of platelet-activating factor (PAF), the antagonists being selected for their apparent structural heterogeneity. The molecules examined were the compact Ginkgolides BN 52020, BN 52021 and BN 52022 (1, 2 and 3), the semi-rigid kadsurenone (4), a flexible synthetic dinor type C furanoid lignan L-652,731 (5a) and the triazolothienobenzodiazepine WEB 2086 (7). Calculation of the electrostatic potential generated around all the above molecules showed the existence of two wells of negative potential or 'cache-oreilles' (ear-muffs), i.e., the isocontours drawn at -10 kcal/mol, located at 180 degrees from each other and separated by a maximum distance of 22-27 A. Except for the synthetic dinor type C furanoid lignan (5a), the molecules also presented a moderate hydrophobic fragment, which constitutes a third point of interaction with the high-affinity binding site in rabbit and human platelets. The findings of the present study allow speculation that this high-affinity acceptor site may be a 'polarized cylinder' with a diameter of 10-12 A. [less ▲]

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