title: Lipid-lowering effects of ethyl 2-phenacyl-3-aryl-1H-pyrrole- 4-carboxylates in rodents.
abstract: 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.
authors.affiliation: Department of Chemistry and Biochemistry, Rider University, 2083 Lawrenceville Rd., Lawrenceville, NJ 08648, USA.
authors.forename: Justin M
authors.initials: JM
authors.lastname: Holub
authors.forename: Kathy
authors.initials: K
authors.lastname: O'Toole-Colin
authors.forename: Adam
authors.initials: A
authors.lastname: Getzel
authors.forename: Anthony
authors.initials: A
authors.lastname: Argenti
authors.forename: Michael A
authors.initials: MA
authors.lastname: Evans
authors.forename: Daniel C
authors.initials: DC
authors.lastname: Smith
authors.forename: Gerard A
authors.initials: GA
authors.lastname: Dalglish
authors.forename: Shahzad
authors.initials: S
authors.lastname: Rifat
authors.forename: Donna L
authors.initials: DL
authors.lastname: Wilson
authors.forename: Brett M
authors.initials: BM
authors.lastname: Taylor
authors.forename: Ulander
authors.initials: U
authors.lastname: Miott
authors.forename: Josephine
authors.initials: J
authors.lastname: Glersaye
authors.forename: Kam Suet
authors.initials: KS
authors.lastname: Lam
authors.forename: Bryan J
authors.initials: BJ
authors.lastname: McCranor
authors.forename: Joshua D
authors.initials: JD
authors.lastname: Berkowitz
authors.forename: Robert B
authors.initials: RB
authors.lastname: Miller
authors.forename: John R
authors.initials: JR
authors.lastname: Lukens
authors.forename: Keith
authors.initials: K
authors.lastname: Krumpe
authors.forename: John T
authors.initials: JT
authors.lastname: Gupton
authors.forename: Bruce S
authors.initials: BS
authors.lastname: Burnham
mesh_terms: D000098:Acetophenones / Q000737:chemistry; D000818:Animals; D000069059:Atorvastatin; D002264:Carboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008076:Cholesterol, HDL / Q000097:blood; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry; D000077340:Fluvastatin; D006538:Heptanoic Acids / Q000737:chemistry; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry; D008077:Lipoproteins, LDL / Q000097:blood; D008297:Male; D051379:Mice; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000098:Acetophenones; D002264:Carboxylic Acids; D008076:Cholesterol, HDL; D005229:Fatty Acids, Monounsaturated; D006538:Heptanoic Acids; D000960:Hypolipidemic Agents; D007211:Indoles; D008077:Lipoproteins, LDL; D011758:Pyrroles; D000077340:Fluvastatin; D000069059:Atorvastatin