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) Synthèse et évaluation pharmacologique de nouvelles benzopyranes en tant qu’activateurs de canaux potassiques sensibles à l’ATP: introduction d’un groupement arylsulfonylurée ou benzothiadiazinedioxyde en position 4; ; et al Poster (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) Dopamine D4 receptors, a new opportunity for research on schizophreniaLiégeois, Jean-François ; ; et alin Current Medicinal Chemistry (1998), 5 Detailed reference viewed: 9 (1 ULg) Tentatives de synthèse énantiosélective des isomères R et S du pirlindolPirotte, Bernard ; De Tullio, Pascal ; et alin Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 12 (1 ULg) Résolution préparative du pirlindol, journées franco-belges de pharmacochimieDe Tullio, Pascal ; ; Liégeois, Jean-François et alin Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 10 (0 ULg) Tentatives de synthèse énantiosélective des isomères R et S du pirlindolePirotte, Bernard ; De Tullio, Pascal ; et alin Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 15 (2 ULg) Design, synthèse et évaluation pharmacologique de nouvelles 2-alkylamino-quinazoline-4-ones en tant du’isostères de 3-alkylamino-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes; ; et al in Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 4 (0 ULg) Design, synthesis and pharmacology of sulfonylcyanoguanidines and sulfonamidonitroethylenes as bioisosteres of hypoglycemic sulfonylureas; ; et al in Journal de Pharmacie de Belgique (1998), 53 Detailed reference viewed: 3 (0 ULg) 4H-1,2,4-Pyridothiadiazine 1,1-dioxides and 2,3-dihydro-4H-1,2,4-pyridothiadiazine 1,1-dioxides chemically related to diazoxide and cyclothiazide as powerful positive allosteric modulators of (R/S)-2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors: design, synthesis, pharmacology and structure-activity relationshipsPirotte, Bernard ; ; et alin Journal of Medicinal Chemistry (1998), 41 Detailed reference viewed: 5 (2 ULg) Design of new potential hypoglycemic drugs; De Tullio, Pascal ; et alin Journal de Pharmacie de Belgique (1998), 53 3-Alkylamino-7-halogeno-4H-1,2,4-benzothiadiazine 1,1-dioxides as new potent KATP channels activatorsDe Tullio, Pascal ; ; et alin European Journal of Pharmaceutical Sciences (1998), suppl.1 Detailed reference viewed: 3 (0 ULg) First preparative enantiomer resolution of pirlindole, a potent antidepressant drugDe Tullio, Pascal ; Felekidis, Apostolos ; Pirotte, Bernard et alin Helvetica Chimica Acta (1998), 81 Detailed reference viewed: 15 (1 ULg) Study of the ring closure reaction of o-aminoarylsulfonamides with 1,1’-thiocarbonyldiimidazoleDe Tullio, Pascal ; Pirotte, Bernard ; et alin Tetrahedron (1998), 54 Detailed reference viewed: 6 (0 ULg) Preparative resolution of racemic pirlindole: chromatographic methods and determination of the absolute configurationDe Tullio, Pascal ; ; Liégeois, Jean-François et alin European Journal of Pharmaceutical Sciences (1998), suppl.1 Detailed reference viewed: 14 (3 ULg) |
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