72826-76-7Relevant 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
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.
Synthesis and diuretic properties of some sulfonylureas related to torasemide
DeLarge,Lapiere,De Ridder,Ghys
, p. 299 - 304 (2007/10/02)
A large number of torasemide-like drugs has been synthesized. The basic structure of 1-alkyl-3-(4-phenylaminopyridin-3-yl)sulfonyl-urea has been modified in view to replace the phenyl group on the 4 position of pyridine nucleus, by groups such as alkylami
