Hypocholesterolemic agents VII: Inhibition of β-hydroxy-β-methylglutaryl-CoA reductase by monoesters of substituted glutaric acids

A series of 1-(4-biphenylyl)pentyl hydrogen 3-alkylglutarates and 3-hydroxy-3-alkylglutarates was synthesized and assayed for inhibition of rat liver β-hydroxy-β-methylglutaryl-CoA reductase. Limited solubility of the monoesters in the enzyme assay system prevented the determination of the I50 value...

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Veröffentlicht in:	Journal of pharmaceutical sciences 1980-05, Vol.69 (5), p.506-509
Hauptverfasser:	Boots, Marvin R., Yeh, Yeong-Maw, Boots, Sharon G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Anticholesteremic Agents - pharmacology Enzyme inhibition-effect of monoesters of glutaric acids on cholesterol biosynthesis Enzyme inhibition—effect of monoesters of glutaric acids on cholesterol biosynthesis, rat liver microsomes Glutarates - pharmacology Hydroxymethylglutaryl-CoA Reductase Inhibitors Hypocholesterolemic agents-inhibition of β-hydroxy-β-methylglutaryl-CoA reductase Hypocholesterolemic agents—inhibition of β-hydroxy-β-methylglutaryl-CoA reductase, monoesters of substituted glutaric acids, rat liver microsomes Microsomes Microsomes, Liver - enzymology Microsomes, rat liver—inhibition of cholesterol biosynthesis, monoesters of substituted glutaric acids monoesters of substituted glutaric acids rat liver microsomes rat liver-inhibition of cholesterol biosynthesis Rats Structure-Activity Relationship
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Zusammenfassung:	A series of 1-(4-biphenylyl)pentyl hydrogen 3-alkylglutarates and 3-hydroxy-3-alkylglutarates was synthesized and assayed for inhibition of rat liver β-hydroxy-β-methylglutaryl-CoA reductase. Limited solubility of the monoesters in the enzyme assay system prevented the determination of the I50 values. However, the limited data indicated no significant changes in the activity of the analogs when they were assayed at identical concentrations.
ISSN:	0022-3549 1520-6017
DOI:	10.1002/jps.2600690507