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  Three-Dimentional Quantitative Structure-Activity Relationships of ATP-Sensitive Potassium (KATP) Channel Openers Belonging to the 3-Alkylamino-4H-1,2,4-benzo- and 3-Alkylamino-4H-1,2,4-pyridothiadiazine 1,1-Dioxide FamiliesDe Tullio, Pascal  ; ; Francotte, Pierre et alin Journal of Medicinal Chemistry (2006), 49 Detailed reference viewed: 5 (0 ULg)Crystal structure of 7-chloro-3-isopropylsulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxide, C10H11CIN2O2S2; ; De Tullio, Pascal et alin Zeitschrift für Kristallographie. New Crystal Structures (2005), NCS 220 Detailed reference viewed: 2 (1 ULg)Crystal structure of 7-chloro-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide, C10H12CIN3O2S; Pirotte, Bernard ; De Tullio, Pascal in Zeitschrift für Kristallographie. New Crystal Structures (2005), NCS 220 Detailed reference viewed: 5 (2 ULg)Crystal structure of 7-chloro-3-isopropoxy-4H-1,2,4-benzothiadiazine 1,1-dioxide monohydrate, C10H13CIN2O4S H2O; ; Pirotte, Bernard et alin Zeitschrift für Kristallographie. New Crystal Structures (2005), NCS 220 Detailed reference viewed: 9 (4 ULg)Improvement of the pharmacophoric model for an agonistic activity of arylthiadiazine dioxides on pancreatic KATP channels using the CoMSIA approachDe Tullio, Pascal ; ; et alPoster (2004, August) Detailed reference viewed: 4 (0 ULg)3-Isopropylamino-7-nitro-1,4,2-benzodithiazine 1,1-dioxide; ; De Tullio, Pascal et alin Acta Crystallographica (2003) Detailed reference viewed: 9 (0 ULg)Original 2-alkylamino-6-halogenoquinazolin-4(3H)-ones and KATP channel activity; ; et al in Journal of Medicinal Chemistry (2001), 44 Detailed reference viewed: 3 (0 ULg)7-Chloro-2-methyl-3-methylamino-2H-1,2,4-benzothiadiazine 1,1-dioxide; ; et al in Acta Crystallographica (2001), E57 Detailed reference viewed: 4 (1 ULg)3-Amino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxide; De Tullio, Pascal ; et alin Acta Crystallographica (2001), E57 Detailed reference viewed: 4 (1 ULg)(R/S)-3-(3-Methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide mono-hydrate; De Tullio, Pascal ; et alin Acta Crystallographica (2001), E57 Detailed reference viewed: 4 (0 ULg)Absolute configuration of N-[(R)-3-methyl-2-butyl]-(S)-2-(6-methoxy-2-naphthyl)-propionamide; ; Pirotte, Bernard et alin Acta Crystallographica (2001), E57 Detailed reference viewed: 6 (1 ULg)3-Alkylamino-4H-pyrido[2,3-e]-1,2,4-thiadiazine 1,1-dioxides structurally related to diazoxide and pinacidil as potassium channel openers acting on vascular smooth muscle cells: design, synthesis and pharmacological evaluationPirotte, Bernard ; ; De Tullio, Pascal et alin Journal of Medicinal Chemistry (2000), 43 Detailed reference viewed: 6 (3 ULg)Crystal structures of R- and S-7-chloro-3-[1-(cyclohexyl)ethylamino]-4H-1,2,4-benzothiadiazine 1,1-dioxide (absolute configurations); De Tullio, Pascal ; et alPoster (1999, October 28) Detailed reference viewed: 2 (0 ULg)7-Iodo-3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxide; Pirotte, Bernard ; De Tullio, Pascal in Acta Crystallographica (1999), C55 Detailed reference viewed: 4 (0 ULg)7-Chloro-(R)-3-[1-(cyclohexyl)ethylamino]-4H-1,2,4-benzothiadiazine 1,1-dioxide and 7-chloro-(S)-3-[1-(cyclohexyl)ethylamino]-4H-1,2,4-benzothiadiazine 1,1-dioxide; De Tullio, Pascal ; et alin Acta Crystallographica (1999), C55 Detailed reference viewed: 7 (3 ULg)4-Ethyl-2,3-dihydro-4H-pyrido[3,2-e]-1,2,4-thiadiazine 1,1-dioxide and 4-ethyl-2,3-dihydro-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide; Pirotte, Bernard ; et alin Acta Crystallographica (1999), C55 Detailed reference viewed: 3 (0 ULg)Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2-butylamino)-4H- and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide, two tissue selective ATP-sensitive potassium channel openers.; De Tullio, Pascal ; et alin Bioorganic & Medicinal Chemistry (1999), 7(8), 1513-20 The preparation and the pharmacological evaluation of the R- and S-isomers of 3-(2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 42) and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4 ... [more ▼] The preparation and the pharmacological evaluation of the R- and S-isomers of 3-(2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 42) and 3-(3-methyl-2-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide (BPDZ 44), two potassium channel openers, is described. Their optical purity was estimated by means of capillary electrophoresis (R- and S-BPDZ 42) and chiral HPLC (R- and S-BPDZ 44). The absolute configuration of each isomer of BPDZ 44 was deduced from crystallographic data. Pharmacological assays performed with the R- and S-isomers of BPDZ 44 revealed only slight differences in their activity on pancreatic B-cells but significant differences in their activity on vascular smooth muscle cells: the R-isomer being sixfold more potent than its corresponding S-isomer. The R-isomer of BPDZ 42 was shown to be more potent than its corresponding S-isomer on the endocrine pancreas. S-BPDZ 44 as well as R- and S-BPDZ 42 were found to exhibit tissue selectivity for the pancreatic versus the vascular smooth muscle tissue. [less ▲] Detailed reference viewed: 13 (1 ULg)Preparation and pharmacological evaluation of the R- and S-enantiomers of 3-(2’-butylamino)-4H- and 3-(3’-methyl-2’-butylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxide, two tissue selective ATP-sensitive potassium channel openers; De Tullio, Pascal ; et alin Bioorganic & Medicinal Chemistry (1999), 7 Detailed reference viewed: 1 (0 ULg)3-Alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potent KATP-channel activators: structural study and influence of stereochemistryDe Tullio, Pascal ; ; et alin Pharmacy and Pharmacology Communications (1999), 5 Detailed reference viewed: 2 (0 ULg) |
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