3-Alkyl-3-hydroxyglutaric Acids: A New Class of Hypocholesterolemic HMG CoA Reductase Inhibitors. 1

JS Baran, I Laos, DD Langford, JE Miller…

文献索引：Baran; Laos; Langford; Miller; Jett; Taite; Rohrbacher Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 597 - 601

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被引用次数: 9

摘要

Derivatives of 3-hydroxy-3-methylglutaric acid (HMG), a portion of the substrate for HMG CoA reductase, were prepared and tested for their inhibitory action against rat liver HMG CoA reductase and for their hypocholesterolemic activity. Structure-dependent competitive inhibition was observed. Optimal structures had a free dicarboxylic acid with an alkyl group of 13-16 carbons at position 3. 3-n-Pentadecyl-3-hydroxyglutaric acid (3j)(ICw= 50 pM) ...