Comparison of the hypolipidemic activity of cyclic vs. acyclic imides.
Two series of nitrogen-substituted cyclic and acyclic imides were examined for hypolipidemic activity in mice after dosing for 16 days at a dose of 20 mg/kg per day. The hypolipidemic activity of the unsubstituted, N-butyl, N-3-oxobutyl, and N-2-carboxyethyl derivatives of diacetimide and succinimide were compared as well as the unsubstituted and N-substituted dibenzimide and diphenimide. It was shown that an imide functionality incorporated into a ring was not necessary for hypocholesterolemic activity. Good hypocholesterolemic activity was observed in both series of acyclic and cyclic imides. However, a cyclic imido structure was a necessary requirement for good hypotriglyceridemic activity. A decrease in hypotriglyceridemic activity was noted when comparing the cyclic imides to their respective acyclic congeners.
D000818:Animals; D002784:Cholesterol / Q000097:blood; D002994:Clofibrate / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis*; D007094:Imides / Q000138:chemical synthesis / Q000494:pharmacology*; D008297:Male; D051379:Mice; D013329:Structure-Activity Relationship; D013388:Succinimides / Q000494:pharmacology; D014280:Triglycerides / Q000097:blood
D000960:Hypolipidemic Agents; D007094:Imides; D013388:Succinimides; D014280:Triglycerides; C032620:succinimide; D002784:Cholesterol; D002994:Clofibrate