Structural study of pinacidil, a potassium channel opener belonging to the chemical class of N-alkyl-N"-cyano-N'-pyridylguanidines

in Helvetica Chimica Acta (1993), 76

A sulfonylthiourea (BM 20) related to torasemide: a new loop diuretic with relative potassium-sparing properties

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 ▲]

Stereoselective hydrogenation of methacycline to doxycycline catalysed by rhodium-carborane complexes

Poster (1992, November)

Application of high performance liquid chromatography to the determination of the optimized reaction conditions giving stereoselective hydrogenation of methacycline to doxycycline

Poster (1992, May 08)

Action of diuretics at the cellular level

in Progress in Pharmacology and Clinical Pharmacology (1992)

Design, Synthesis and Biological Activity of a Series of Torasemide Derivatives, Potent Blockers of the Na+ 2cl- K+ Co-Transporter: In-Vitro Study

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 ▲]

Synthèse, étude théorique et évaluation biologique de dérivés du 4-amino-4H-1,2,4-triazole analogues des antibiotiques b-lactamiques

in European Journal of Medicinal Chemistry (1992), 27(3), 193-205

New relative K+-sparing high ceiling diuretics related to torasemide

in Journal de Pharmacie de Belgique (1992), 47

4-Amino-4H-1,2,4-triazole and 5-aminothiazole derivatives structurally related to β-lactam antibiotics as potential inhibitors of serine proteases

Poster (1991, September 19)

Loop diuretics : SAR, molecular interactions and target topography

Poster (1991, September)