Hypocholesterolemic Agents II: Inhibition of β-Hydroxy-β-methylglutaryl Coenzyme A Reductase by Arylalkyl Hydrogen Succinates and Glutarates

Autor:	Marvin R. Boots, Kenneth E. Guyer, Carole M. Noble, Sharon G. Boots
Rok vydání:	1973
Předmět:	Hydrogen Chemistry Stereochemistry Anticholesteremic Agents Coenzyme A Pharmaceutical Science chemistry.chemical_element Succinates Cooperativity Saccharomyces cerevisiae Reductase Glutarates Yeast Kinetics chemistry.chemical_compound Spectrophotometry Oxidoreductases Dialysis
Zdroj:	Journal of Pharmaceutical Sciences. 62:952-957
ISSN:	0022-3549
Popis:	A series of arylalkyl hydrogen succinates and glutarates was synthesized and assayed for inhibition of yeast β -hydroxy- β - methylglutaryl coenzyme A reductase. The following compounds were found to be particularly active as inhibitors: l-(4-biphenylyl)- pentyl hydrogen succinate (5S), l-(4-biphenylyl)-hexyl hydrogen succinate (6S), l-(4-biphenylyl)-pentyl hydrogen glutarate (5G), 1-(2-fluorenyl)-pentyl hydrogen succinate (13S), and l-(2-fluorenyl)- pentyl hydrogen glutarate (13G). Further studies with Compound 5S indicated that the inhibition was reversible and noncompetitive with respect to β -hydroxy- β -methylglutaryl coenzyme A and NADPH. Dixon and modified Hill plots were used to calculate a cooperativity number of 3 for 5S.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ca93c26041e8c07f6daa14aa512ba70 https://doi.org/10.1002/jps.2600620620 Zobrazit plný text záznamu Plný text