Pharmacomodulation of 7-(2-methylene-butyryl)-2,3-dihydrobenzoxazin-[1,4]-3-one structure and normolipemic activity.
A series of compounds from 7-(2-methylene butyryl)-2,3-dihydro benzoxazin-[1,4]-3-one was synthesized and evaluated for its lipid lowering action in animal models. Substitutions in positions 2, 4 and 7 were performed. The results of the structure-activity relationships are very difficult to be interpreted. The different modifications tested did not show any improvement in the normolipemic activity.
Moussavi
Z
Z
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Lille, France.
Depreux
P
P
Lesieur
D
D
Cotelle
N
N
Sauzieres
J
J
Plancke
M O
MO
Fruchart
J C
JC
D000818:Animals; D001835:Body Weight / Q000187:drug effects; D002087:Butyrates / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D056486:Chemical and Drug Induced Liver Injury / Q000503:physiopathology; D005260:Female; D000960:Hypolipidemic Agents / Q000138:chemical synthesis*; D008055:Lipids / Q000097:blood; D008297:Male; D051379:Mice; D008830:Microbodies / Q000187:drug effects; D010078:Oxazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D002087:Butyrates; D000960:Hypolipidemic Agents; D008055:Lipids; D010078:Oxazines