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 sev...

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Veröffentlicht in:	Journal of medicinal chemistry 1985-06, Vol.28 (6), p.815-818
Hauptverfasser:	Cascio, Giuseppe, Manghisi, Elso, Porta, Roberto, Fregnan, Giancarlo
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticholesteremic Agents - chemical synthesis Chemistry Cholesterol - analysis Clofibrate - pharmacology Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Lipoproteins - blood Mice Mice, Inbred Strains Organic chemistry Piperazines - chemical synthesis Piperazines - pharmacology Preparations and properties Rats Rats, Inbred Strains Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00383a021