Article (Scientific journals)
Design, 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.
1992In Journal of Pharmacy and Pharmacology, 44, p. 589-593
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Abstract :
[en] 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.
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Masereel, B.
Lohrmann, E.
Schynts, M.
Pirotte, Bernard ;  Université de Liège - ULiège > Chimie pharmaceutique
Greger, R.
Delarge, J.
Language :
English
Title :
Design, Synthesis and Biological Activity of a Series of Torasemide Derivatives, Potent Blockers of the Na+ 2cl- K+ Co-Transporter: In-Vitro Study
Publication date :
1992
Journal title :
Journal of Pharmacy and Pharmacology
ISSN :
0022-3573
eISSN :
2042-7158
Publisher :
Wiley, London, United Kingdom
Volume :
44
Pages :
589-593
Peer reviewed :
Peer Reviewed verified by ORBi
Available on ORBi :
since 07 December 2009

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