137783-13-2Relevant academic research and scientific papers
Synthesis and pharmacology of pyrid-3-yl sulfonylureas and thioureas as astrocytic Na+2Cl-K+ cotransporter inhibitors
Masereel, B.,Renard, P.,Schynts, M.,Pirotte, B.,Tullio, P. de,Delarge, J.
, p. 527 - 536 (2007/10/02)
The pharmacology of lipophilic 4-arylamino- and 4-cycloalkylaminopyrid-3-ylsulfonyl(thio)ureas and their synthesis designed from torasemide are described.These compounds could lead to a method of inhibiting the astrocytic Na+2Cl-Ksu
Pyridylsulfonylurea and pyridylsulfonylthiourea compounds
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, (2008/06/13)
The invention concerns a compound of formula (I) STR1 in which: R represents cycloalkyl, bicycloalkyl or polycycloalkyl, X represents oxygen or sulfur, and R1 represents alkyl, cycloalkyl, bicycloalkyl, or polycycloalkyl. Medicaments thereof and use of sa
Design, synthesis and biological activity of a series of torasemide derivatives, potent blockers of the Na+ 2Cl- K+ co-transporter: In-vitro study
Masereel,Lohrmann,Schynts,Pirotte,Greger,Delarge
, p. 589 - 593 (2007/10/02)
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.
