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Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents

Author(s): Justin M. Holub | Kathy O'Toole-Colin | Adam Getzel | Anthony Argenti | Michael A. Evans | Daniel C. Smith | Gerard A. Dalglish | Shahzad Rifat | Donna L. Wilson | Brett M. Taylor | Ulander Miott | Josephine Glersaye | Kam Suet Lam | Bryan J. McCranor | Joshua D. Berkowitz | Robert B. Miller | John R. Lukens | Keith Krumpe | John T. Gupton | Bruce S. Burnham

Journal: Molecules
ISSN 1420-3049

Volume: 9;
Issue: 3;
Start page: 134;
Date: 2004;
Original page

Keywords: Pyrrole | hypolipidemia | cholesterol | triglyceride

A series of substituted 2-phenacyl-3-phenyl-1H-pyrrole-4-carboxylates were prepared from substituted acetophenones in 6 steps. The final condensations between a chloroenal and an aminoketone were carried out under neutral conditions in parallel to yield the series listed below. Selected pyrrole derivatives proved to be potent hypolipidemic agents lowering serum triglyceride concentrations in CF-1 male mice after 14 days of I.P. administration. One agent orally lowered serum cholesterol in Sprague-Dawley male rats at 2mg/kg/day after 14 days. The agents demonstrated a lowering of mouse serum LDL- cholesterol levels and selected compounds showed an elevation of serum HDL-cholesterol levels. The cholesterol concentrations in the liver were raised while the cholesterol and triglyceride contents of the aorta were significantly lowered by the selected trisubstituted pyrrole.
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