Les activateurs de canaux potassiques: étude structurale comparative du pinacidil, du diazoxide et du cromakalimDupont, Léon ; Pirotte, Bernard ; De Tullio, Pascal et alin Annales Pharmaceutiques Françaises (1995), 53(5), 201-8 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 ▲] Detailed reference viewed: 17 (1 ULg) Synthèse de dérivés originaux de la classe des 1,2,4-pyridothiadiazine 1,1-dioxydes : Potentialités pharmacologiques et thérapeutiquessDe Tullio, Pascal ![]() Doctoral thesis (1995) Detailed reference viewed: 6 (0 ULg) Comparative effect of various potassium channel openers on the firing rate of hippocampal and dopaminergic neurons in vitroScuvée-Moreau, Jacqueline ; Seutin, Vincent ; Pirotte, Bernard et alin Pflügers Archiv : European Journal of Physiology (1995), 430 Detailed reference viewed: 15 (11 ULg) 3-Arylcarboxamidométhyl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes en tant qu'antagonistes non peptidiques de la cholécystokinine: synthèse et évaluation pharmacologiquePirotte, Bernard ; De Tullio, Pascal ; et alin Journal de Pharmacie de Belgique (1995), 50 Detailed reference viewed: 5 (1 ULg) ATP-sensitive K+ channels and insulin release: effect of BPDZ 62; ; et al in Diabetologia (1995), 38 Detailed reference viewed: 4 (1 ULg) 7-Methyl-3-methylthio-4H-pyrido[4,3-e]-1,2,4-thiadiazin-7-ium-4-ide 1,1-dioxide zwitterion; De Tullio, Pascal ; Pirotte, Bernard et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 3 (0 ULg) Pyrido- and benzothiadiazinedioxides structurally related to diazoxide: new activators of the pancreatic and vascular KATP channelsDe Tullio, Pascal ; Pirotte, Bernard ; et alin Pflügers Archiv : European Journal of Physiology (1995), 430 Detailed reference viewed: 5 (0 ULg) 3-Methyl-4H-pyrido[4,3-e][1,2,4]thiadiazine 1,1-dioxide monohydrate; De Tullio, Pascal ; Pirotte, Bernard et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 7 (1 ULg) N2-cyano-N1-isopropyl-N3-[4-(3-methylphenylamino)-3-pyridylsulfonyl]guanidine; ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 10 (0 ULg) Synthesis and pharmacology of pyrid-3-ylsulfonylcyanoguanidines as diuretics; ; et al in European Journal of Medicinal Chemistry (1995), 30 Detailed reference viewed: 16 (0 ULg) 2,4,7-Trimethyl-2,3-dihydro-4H-pyrido[4,3-e]-1,2,4-thiadiazinium 1,1-dioxide iodide; Pirotte, Bernard ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 4 (0 ULg) 3-Methyl-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxide; Pirotte, Bernard ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 3 (2 ULg) 3-Methyl-4H-pyrido[3,2-e][1,2,4]thiadiazine 1,1-dioxide; Pirotte, Bernard ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 4 (1 ULg) Synthesis ans structural studies of a new class of heterocyclic compounds: 1,2,4-pyridothiadiazine 1,1-dioxides, pyridyl analogues of 1,2,4-benzothiadiazine 1,1-dioxidesDe Tullio, Pascal ; Pirotte, Bernard ; et alin Tetrahedron (1995), 51 Detailed reference viewed: 3 (1 ULg) Synthesis and pharmacology of N"-(4-arylaminopyrid-3-yl)sulfonyl-N-cyano-N'-isopropyl-guanidines; ; Pirotte, Bernard et alin Journal de Pharmacie de Belgique (1995), 50 Detailed reference viewed: 5 (1 ULg) Synthèse de dérivés 3-aminoaralkyl-2-aryl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxydes et leur évaluation en tant qu'antagonistes de la cholécystokinineDe Tullio, Pascal ; Pirotte, Bernard ; et alin Journal de Pharmacie de Belgique (1995), 50 Detailed reference viewed: 3 (1 ULg) 3,7-Dimethyl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide zwitterion; Pirotte, Bernard ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 2 (0 ULg) 3-Benzamido-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide; De Tullio, Pascal ; Pirotte, Bernard et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 7 (2 ULg) Les activateurs de canaux potassiques: étude structurale comparative du pinacidil, du diazoxide et du cromakalim; Pirotte, Bernard ; De Tullio, Pascal et alin Annales Pharmaceutiques Françaises (1995), 53 Detailed reference viewed: 16 (2 ULg) 3-amino-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide monohydrate and 3-tert-butyl-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide; Pirotte, Bernard ; De Tullio, Pascal et alin Acta Crystallographica (1995), C51 Detailed reference viewed: 4 (0 ULg) |
||