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See detailCoupling of Liquid Chromatography/Tandem Mass Spectrometry and Liquid Chromatography/Solid-Phase Extraction/NMR Techniques for the Structural Identification of Metabolites following In Vitro Biotransformation of SUR1-Selective ATP-Sensitive Potassium Channel Openers
Gillotin, F.; Chiap, Patrice ULg; Frederich, Michel ULg et al

in Drug Metabolism and Disposition : The Biological Fate of Chemicals (2010), 38(2), 232-240

SUR1-selective ATP-sensitive potassium channel openers (PCOs) have been shown to be of clinical value for the treatment of several metabolic disorders, including type I and type II diabetes, obesity and ... [more ▼]

SUR1-selective ATP-sensitive potassium channel openers (PCOs) have been shown to be of clinical value for the treatment of several metabolic disorders, including type I and type II diabetes, obesity and hyperinsulinemia. Taking into account these promising therapeutic benefits, different series of 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides structurally related to diazoxide were developed. In view of the lead optimisation process of the series, knowledge of ADMET parameters, and more particularly the metabolic fate of these compounds, is a fundamental requirement. For such a purpose, two selected promising compounds (BPDZ 73 and BPDZ 157) were incubated in the presence of phenobarbital-induced rat liver microsomes to produce expected mammal in vivo phase I metabolites. The resulting major metabolites were then analysed by both MS and NMR in order to completely elucidate their chemical structures. The two compounds were also further incubated in the presence of non-treated rats and human microsomes in order to compare the metabolic profiles. In the present study, the combined use of an exact mass LC-MS/MS platform and a LC-SPE-NMR system allowed the clarification of some unresolved structural assessments in the accurate chemical structure elucidation process of the selected PCOs drugs. These results greatly help the optimization of the lead compounds. [less ▲]

Detailed reference viewed: 109 (39 ULg)
See detailApplication of LC-SPE-NMR to the structural determination of metabolites of KATP channel openers belonging to 3-alkylamino-4H-1,2,4-arylthiadiazine 1,1-dioxides
Francotte, Pierre ULg; Gillotin, F.; Van Heuguen, J. C. et al

Conference (2007, October)

Detailed reference viewed: 3 (1 ULg)
See detailIn vitro metabolisation study of several 3-alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers : combined use of LC-Q-TOF MS/MS and LC-SPE-NMR
De Tullio, Pascal ULg; Chiap, Patrice ULg; Francotte, Pierre ULg et al

Poster (2006, November 18)

Detailed reference viewed: 6 (1 ULg)
See detailCombined use of LC-SPE-NMR and LC-MS for the metabolites characterization of ATP-sensitive potassium channel openers belonging to 3-alkylamino-4H-1,2,4-arylthiadiazine 1,1-dioxides
De Tullio, Pascal ULg; Gillotin, F.; Francotte, Pierre ULg et al

Poster (2006, August)

Detailed reference viewed: 9 (0 ULg)
See detailApplication de la LC-SPE-RMN et de la LC-MS à la détermination structurale des métabolites d’activateurs des canaux KATP de la classe des 3-alkylamino-4H-arylthiadiazine 1,1-dioxydes
De Tullio, Pascal ULg; Chiap, Patrice ULg; Francotte, Pierre ULg et al

Poster (2006, June)

Detailed reference viewed: 45 (2 ULg)
See detailApplication of LC-SPE-NMR and LC-Q-TOF MS/MS to the structural determination of KATP channel openers metabolites belonging to the 3-alkylamino-4H-1,2,4-arylthiadiazine 1,1-dioxides
Gillotin, F.; De Tullio, Pascal ULg; Van Heugen, Jean-Claude ULg et al

Poster (2006, May 17)

Detailed reference viewed: 14 (1 ULg)