Lipid-Lowering Effects of Ethyl 2-Phenacyl-3-aryl-1H-pyrrole-4-carboxylates in Rodents
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 2 mg/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.
Holub, Justin M.,O'Toole-Colin, Kathy,Getzel, Adam,Argenti, Anthony,Evans, Michael A.,Smith, Daniel C.,Dalglish, Gerard A.,Rifat, Shahzad,Wilson, Donna L.,Taylor, Brett M.,Miott, Ulander,et al.
p. 135 - 157
(2007/10/03)
Application of 2-Substituted Vinamidinium Salts to the Synthesis of 2,4-Disubstituted Pyrroles
A variety of 2-substituted vinamidinium salts react with α-amino acid esters under basic conditions to produce 2-carbethoxy-4-substituted-pyrroles in good yield.The overall process represents a short and efficient synthesis of highly functionalized pyrrol
Gupton, John T.,Krolikowski, Dale A.,Yu, Richard H.,Riesinger, Steve W.,Sikorski, James A.
p. 4735 - 4740
(2007/10/02)
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