References of "Pirotte, Bernard"
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See detailLoop diuretics and the renal Na+K+2Cl- cotransport: interaction model
Masereel, B.; Schynts, M.; Pirotte, Bernard ULg et al

Conference (1993, March)

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See detailStereoselective hydrogenation of methacycline to doxycycline catalysed by rhodium-carborane complexes
Pirotte, Bernard ULg; Felekidis, Apostolos ULg; Fontaine, M. et al

in Tetrahedron Letters (1993), 34

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See detailImproved pancreatic K-ATP channel openers belonging to the pyridothiadiazine chemical class
Pirotte, Bernard ULg; De Tullio, Pascal ULg; Lebrun, P. et al

in Journal de Pharmacie de Belgique (1993), 48

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See detailBPDZ 44: a new and potent activator of ATP-sensitive K+ channels
Lebrun, P.; Pirotte, Bernard ULg; Antoine, M.-H. et al

in Diabetologia (1993), 36

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See detailLoop diuretics and the renal Na+K+2Cl- cotransport: interaction model
Masereel, B.; Schynts, M.; Pirotte, Bernard ULg et al

in Journal de Pharmacie de Belgique (1993), 48

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See detailA sulfonylthiourea (BM 20) related to torasemide: a new loop diuretic with relative potassium-sparing properties
Masereel, B.; Schynts, M.; Krzesinski, Jean-Marie ULg et al

in Journal of Pharmacy & Pharmacology (1993), 45

A series of sulphonylthioureas related to torasemide, a high ceiling loop diuretic, were synthesized and found to inhibit the Na+ 2Cl- K+ co-transporter of the thick ascending limb of the loop of Henlé ... [more ▼]

A series of sulphonylthioureas related to torasemide, a high ceiling loop diuretic, were synthesized and found to inhibit the Na+ 2Cl- K+ co-transporter of the thick ascending limb of the loop of Henlé. Their diuretic properties were studied (30 mg kg-1) after oral administration to rats. Lipophilic derivatives very active in-vitro, were found inactive orally and intraperitoneally in rats. The four most active compounds were examined for their dose-dependent diuresis. Three of them showed a potency, water and electrolyte excretion similar to torasemide. The fourth molecule, a sulphonylthiourea (BM 20), exhibited relative potassium-sparing properties and a minimal diuretic dose of 0.001 mg kg-1, 200 times lower than torasemide. [less ▲]

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See detailNew dihydrocoumarine derivatives as potential mechanism-based inactivators of serine proteinases
Schynts, M.; Boggetto, N.; Masereel, B. et al

Poster (1992, November 06)

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See detailStereoselective hydrogenation of methacycline to doxycycline catalysed by rhodium-carborane complexes
Fontaine, M.; Demonceau, Albert ULg; Noëls, A. F. et al

Poster (1992, November)

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See detailsynthesis of sulfonylthioureas related to torasemide as new "high ceiling diuretics
Masereel, B.; Schynts, M.; Pirotte, Bernard ULg et al

Poster (1992, July)

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See detailNew relative K+-sparing high ceiling diuretics related to torasemide
Masereel, B.; Schynts, M.; Lohrmann, E. et al

Conference (1992)

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See detailAction of diuretics at the cellular level
Lohrmann, E.; Masereel, B.; Nitschke, R. et al

in Progress in Pharmacology and Clinical Pharmacology (1992)

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See detailNew dihydrocoumarine derivatives as potential mechanism-based inactivators of serine proteinases
Schynts, M.; Boggetto, N.; Masereel, B. et al

in Pharmaceutisch Weekblad (1992), 14

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See detailDesign, Synthesis and Biological Activity of a Series of Torasemide Derivatives, Potent Blockers of the Na+ 2cl- K+ Co-Transporter: In-Vitro Study
Masereel, B.; Lohrmann, E.; Schynts, M. et al

in Journal of Pharmacy & Pharmacology (1992), 44

Pharmacomodulation of the torasemide molecule, a loop diuretic inhibiting Na+ 2Cl- K+ co-transport in the thick ascending limb of the loop of Henle has been performed in order to obtain new long-acting ... [more ▼]

Pharmacomodulation of the torasemide molecule, a loop diuretic inhibiting Na+ 2Cl- K+ co-transport in the thick ascending limb of the loop of Henle has been performed in order to obtain new long-acting diuretics. The aim of this study was to decrease the metabolism of the drug and to slow down its rate of excretion by increasing its hydrophobicity. The present study describes the synthesis and the inhibitory potency of new torasemide derivatives in the bioassay system of the cortical thick ascending limb of rabbit. A correlation between the lipophilicity (log P') of these substances and their activity as inhibitors of the Na+ Cl- K+ co-transporter was observed. The present design led to compounds more active than torasemide. Structure-activity relationships permit us to propose an interaction model between torasemide derivatives and the Na+ 2Cl- K+ co-transport system of the cortical thick ascending limb. [less ▲]

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