N-phenylpiperazine derivatives with hypocholesterolemic activity.
A series of new 4-(4-phenyl-1-piperazinyl)-1-(4-fluorophenyl)-2-(acyloxy)-1-butanones and 4-aryl-5-[omega-(4-aryl-1-piperazinyl)alkyl]-1,3-dioxol-2-ones were synthesized and tested preliminarily for hypolipemic activity. Plasma cholesterol-lowering activity in normal rats was found especially in several dioxolones, two of the most active compounds (6 and 8) being more potent than clofibrate. 4-(4-Chlorophenyl)-5-[2-(4-phenyl-1-piperazinyl)ethyl]-1,3-dioxol- 2-one (8, LR-19,731) has been selected for clinical trials.
D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis; D002784:Cholesterol / Q000032:analysis; D002994:Clofibrate / Q000494:pharmacology; D008074:Lipoproteins / Q000097:blood; D051379:Mice; D008815:Mice, Inbred Strains; D010879:Piperazines / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship
D000924:Anticholesteremic Agents; D008074:Lipoproteins; D010879:Piperazines; D002784:Cholesterol; D002994:Clofibrate; C031503:phenylpiperazine