Design, synthesis and biological evaluation of sulfonylureas as original non-prostanoïd thromboxane A2 receptor antagonists; ; et al Conference (1998, November 27) Detailed reference viewed: 3 (0 ULg) Design, synthesis and biological evaluation of sulfonylureas as original non-prostanoid thromboxane A2 receptor antagonists; ; et al Poster (1998, November 27) Detailed reference viewed: 5 (0 ULg) Pharmacological study of original 3-alkylamino-2-methyl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides; ; et al Poster (1998, November 21) Detailed reference viewed: 2 (0 ULg) Simultaneous Determination of Pirlindole Enantiomers and Dehydropirlindole by Chiral Liquid ChromatographyCeccato, Attilio ; Hubert, Philippe ; De Tullio, Pascal et alin Journal of Pharmaceutical & Biomedical Analysis (1998), 17(6-7), 1071-9 Liquid chromatography was employed for the determination of pirlindole enantiomers and its oxidation product dehydropirlindole (DHP). The direct separation of pirlindole enantiomers and DHP was achieved ... [more ▼] Liquid chromatography was employed for the determination of pirlindole enantiomers and its oxidation product dehydropirlindole (DHP). The direct separation of pirlindole enantiomers and DHP was achieved on a cellulose tris-(3,5-dimethylphenylcarbamate) chiral stationary phase (Chiralcel OD-R). Acetonitrile was used as the organic modifier and sodium perchlorate was used as an ionic additive in the mobile phase. The influence of acetonitrile and sodium perchlorate concentrations on enantioselectivity and achiral selectivity towards DHP was investigated in order to find suitable conditions for the determination of low amounts of each analyte. The mobile phase selected consisted of a mixture of acetonitrile and phosphate buffer (pH 5.0) containing sodium perchlorate (0.05 M) (35:65, v/v) and the UV detector was set at 220 nm. The method developed was validated and was found to be linear in the 0.1-5 microg ml(-1) range (r2 = 0.999 for the three compounds). Repeatability and the intermediate precision for the three analytes at a concentration of 0.1 microg ml(-1) were about 3 and 4%, respectively. This concentration corresponds to the quantification of 0.1% for the minor enantiomer. Actual determinations of enantiomeric purity for single enantiomers of pirlindole were performed. [less ▲] Detailed reference viewed: 11 (2 ULg) Effective resolution of racemic pirlindole at the preparative scale: derivatization method and absolute configurationDe Tullio, Pascal ; Ceccato, Attilio ; Liégeois, Jean-François et alPoster (1998, September) Detailed reference viewed: 18 (1 ULg) Preparative resolution of racemic pirlindole: chromatographic methods and determination of the absolute configurationDe Tullio, Pascal ; Ceccato, Attilio ; Liégeois, Jean-François et alPoster (1998, September) Detailed reference viewed: 5 (0 ULg) 3-Alkylamino-7-halogeno-4H-1,2,4-benzothiadiazine 1,1-dioxides as new potent KATP channels activatorsDe Tullio, Pascal ; ; et alPoster (1998, September) 2,3-Dihydro-4H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA) receptorsPirotte, Bernard ; ; et alPoster (1998, September) Detailed reference viewed: 2 (0 ULg) Synthesis and biological evaluation of the 3-alkylamino-7-halogeno-4H-1,2,4-benzothiadiazine 1,1-dioxides: new potential KATP channels openersDe Tullio, Pascal ; ; et alPoster (1998, September) Detailed reference viewed: 1 (0 ULg) Les 3-alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes en tant quactivateurs de canaux KATP: étude structurale et influence de la stéréochimieDe Tullio, Pascal ; ; et alConference (1998, May) Detailed reference viewed: 3 (0 ULg) Les arylthiadiazinedioxydes en tant qu’activateurs des canaux potassiques: etude pharmacologique des 3-alkylamino-2-méthyl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes; ; et al Poster (1998, May) Detailed reference viewed: 1 (0 ULg) Les 3-alkylamino[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes en tant qu’activateurs des canaux KATP: détermination de la position de la liaison double du cycle thiadiazineDe Tullio, Pascal ; ; et alPoster (1998, May) Detailed reference viewed: 3 (0 ULg) Utilisation du 1,1’-thiocarbonyldiimidazole comme agent de cyclisation des aminoarylsulfonamides en vue de l’obtention d’intermédiaires utilisables dans la synthèse de nouveaux activateurs de canaux KATP; Pirotte, Bernard ; et alPoster (1998, May) Detailed reference viewed: 6 (0 ULg) Résolutions énantiomériques et évaluations biologiques des isomères du BPDZ 42 et du BPDZ 44De Tullio, Pascal ; ; Fillet, Marianne et alPoster (1998, May) Detailed reference viewed: 1 (0 ULg) Les 3-alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxydes structuralement apparentés au diazoxide et au pinacidil: conception, synthèse et évaluation biologiquePirotte, Bernard ; ; De Tullio, Pascal et alPoster (1998, May) Detailed reference viewed: 2 (1 ULg) New quinazolinones structurally related to diazoxide and pinacidil as potential KATP channel openers; ; De Tullio, Pascal et alConference (1998, February 14) Detailed reference viewed: 2 (0 ULg) Nouvelles 2-alkylamino-quinazoline-4-ones, synthèse et évaluation pharmacologique en tant qu’isostères potentiels de 3-alkylamino-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes; ; et al Conference (1998, January 16) Detailed reference viewed: 1 (0 ULg) Séparation énantiomérique du pirlindole à l’échelle préparativeDe Tullio, Pascal ; ; Felekidis, Apostolos et alPoster (1998, January 16) Detailed reference viewed: 4 (0 ULg) Comparative study of pirlindole, a selective RIMA, and its two enantiomers using biochemical and behavioural techniques.; Liégeois, Jean-François ; et alin Behavioural Pharmacology (1998), 9(8), 731-7 The interaction with monoamine oxidase A (MAO-A) and B has been shown to be sensitive to the absolute configuration of molecules. Therefore, the aim of this study was to compare the effects of the racemic ... [more ▼] The interaction with monoamine oxidase A (MAO-A) and B has been shown to be sensitive to the absolute configuration of molecules. Therefore, the aim of this study was to compare the effects of the racemic pirlindole (a selective and reversible MAO-A inhibitor) and its two enantiomers using biochemical techniques (in vitro and ex vivo determination of rat brain MAO-A and MAO-B activity) and behavioural models (forced swimming test and reserpine-induced hypothermia and palpebral ptosis test). In vitro, the MAO-A IC50 of (+/-)-pirlindole, R-(-)-pirlindole and S-(+)-pirlindole were 0.24, 0.43 and 0.18 microM, respectively. Ex vivo, their ID50 were 24.4, 37.8 and 18.7 mg/kg i.p. The differences between the three compounds were not significant, with a ratio between the two enantiomers [R-(-)/S-(+)] of 2.2 in vitro and 2.0 ex vivo. MAO-B was only slightly inhibited. In the forced swimming test and the reserpine-induced hypothermia and ptosis model, the three compounds had an antidepressant profile. In the forced swimming test, the minimal effective dose ratio between the R-(-) and the S-(+) was again around 2.0. The behavioural observations were thus clearly in accordance with the biochemical data. [less ▲] Detailed reference viewed: 22 (2 ULg) Liquid chromatographic separation of pirlindole enantiomers using different types of chiral stationary phasesCeccato, Attilio ; Hubert, Philippe ; De Tullio, Pascal et alin Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 7 (0 ULg) |
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