Lipid-lowering properties of 6-benzoyl-2(3H)-benzothiazolone and structurally related compounds.
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.
Yous
Saïd
S
Laboratoire de Chimie Thérapeutique, EA 1043, Faculté des Sciences Pharmaceutiques et Biologiques de Lille, 3 rue du Professeur Laguesse, B. P. 83 59006, Lille Cedex, France.
Lebegue
Nicolas
N
Poupaert
Jacques-Henry
JH
Chavatte
Philippe
P
Berthelot
Pascal
P
D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001835:Body Weight / Q000187:drug effects; D004032:Diet; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005260:Female; D006937:Hypercholesterolemia / Q000097:blood / Q000188:drug therapy*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008055:Lipids / Q000097:blood; D051379:Mice; D015394:Molecular Structure; D009929:Organ Size / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
C508698:6-benzoyl-2(3H)-benzothiazolone; D052160:Benzothiazoles; D000960:Hypolipidemic Agents; D008055:Lipids; D013844:Thiazoles