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Lipid-lowering properties of 6-benzoyl-2(3H)-benzothiazolone and structurally related compounds.

Abstract
Fifteen compounds derived from the 2(3H)-benzothiazolone template with an acyl side-chain in position-6 were evaluated for their lipid-lowering action in mice. Among these compounds, 6-benzoyl-2(3H)-benzothiazolone was found to be the most potent one both in mice models receiving a hypercholesterolemic diet (for 15 days) or a standard diet (for 21 days). 6-Benzoyl-2(3H)-benzothiazolone compares favorably with fenofibrate, the standard drug, both in terms of HDL-C/Chol (High Density Lipoprotein-Cholesterol/Total Cholesterol) ratio and absence of liver hepatomegaly.
AuthorsSaïd Yous, Nicolas Lebegue, Jacques-Henry Poupaert, Philippe Chavatte, Pascal Berthelot
JournalJournal of enzyme inhibition and medicinal chemistry (J Enzyme Inhib Med Chem) Vol. 20 Issue 6 Pg. 525-32 (Dec 2005) ISSN: 1475-6366 [Print] England
PMID16408788 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • 6-benzoyl-2(3H)-benzothiazolone
  • Benzothiazoles
  • Hypolipidemic Agents
  • Lipids
  • Thiazoles
Topics
  • Animals
  • Benzothiazoles (chemical synthesis, chemistry, pharmacology)
  • Body Weight (drug effects)
  • Diet
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Female
  • Hypercholesterolemia (blood, drug therapy)
  • Hypolipidemic Agents (chemical synthesis, chemistry, pharmacology)
  • Lipids (blood)
  • Mice
  • Molecular Structure
  • Organ Size (drug effects)
  • Thiazoles (chemical synthesis, chemistry, pharmacology)

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