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Open AccessArticle

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

Department of Chemistry and Biochemistry, Rider University, 2083 Lawrenceville Rd., Lawrenceville, NJ 08648, USA
Department of Chemistry, University of Richmond, Richmond, VA 23173, USA
Department of Chemistry, UNC-Asheville, One University Heights, Asheville, NC 28801, USA
Author to whom correspondence should be addressed.
Molecules 2004, 9(3), 134-157;
Published: 28 February 2004
(This article belongs to the Special Issue Biologically Relevant Heterocyclic Compounds)
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. View Full-Text
Keywords: Pyrrole; hypolipidemia; cholesterol; triglyceride Pyrrole; hypolipidemia; cholesterol; triglyceride
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Holub, J.M.; O'Toole-Colin, K.; Getzel, A.; Argenti, A.; Evans, M.A.; Smith, D.C.; Dalglish, G.A.; Rifat, S.; Wilson, D.L.; Taylor, B.M.; Miott, U.; Glersaye, J.; Lam, K.S.; McCranor, B.J.; Berkowitz, J.D.; Miller, R.B.; Lukens, J.R.; Krumpe, K.; Gupton, J.T.; Burnham, B.S. Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in Rodents. Molecules 2004, 9, 134-157.

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