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See detailPreparation 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
Khelili, S.; De Tullio, Pascal ULg; Lebrun, P. et al

in Bioorganic & Medicinal Chemistry (1999), 7(8), 1513-1520

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 ▲]

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See detailPharmacological evaluation of 3-alkylsulfanyl-4H-1,2,4-benzothiadiazine 1,1-dioxides structurally related to the KATP channel opener diazoxide
Boverie, S.; Nguyen, Q.-A.; De Tullio, Pascal ULg et al

in Fundamental & Clinical Pharmacology (1999), 13

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See detailIn vivo et in vitro effect of new glibenclamide isosteres
Lebrun, P.; Ouedraogo, R.; Nguyen, Q.-A. et al

in Fundamental & Clinical Pharmacology (1999), 13, Suppl. 1

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See detailSynthesis and pharmacological evaluation of KATP-channel openers related to cromakalim: introduction of arylsulphonylurea moieties
Khelili, S.; Nguyen, Q.-A.; Lebrun, P. et al

in Pharmacy and Pharmacology Communications (1999), 5

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See detailPharmacological study of original 3-alkylamino-2-methyl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides
Ouedraogo, R.; Nguyen, Q.-A.; Antoine, M.-H. et al

in Fundamental & Clinical Pharmacology (1999), 13

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See detailNew 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as putative KATP channel openers: design, synthesis and pharmacological evaluation
Somers, F.; De Tullio, Pascal ULg; Boverie, S. et al

in Fundamental & Clinical Pharmacology (1999), 13

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See detail3-Alkylamino-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potent KATP-channel activators: structural study and influence of stereochemistry
De Tullio, Pascal ULg; Khelili, S.; Ouedraogo, R. et al

in Pharmacy and Pharmacology Communications (1999), 5

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See detailIn vivo and in vitro effect of new glibenclamide isosteres
Nguyen, Q. A.; Ouedraogo, R.; Antoine, M. H. et al

Conference (1998, December 12)

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See detailPharmacological study of original 3-alkylamino-2-methyl-2H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides
Ouedraogo, R.; Nguyen, Q. A.; Antoine, M. H. et al

Poster (1998, November 21)

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See detailNew quinazolinones structurally related to diazoxide and pinacidil as potential KATP channel openers
Somers, F.; Ouedraogo, R.; De Tullio, Pascal ULg et al

Conference (1998, February 14)

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