Abstract
A series of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)- enoates (-heptanoates) 1 and 2 have been prepared and tested for inhibiti 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The most potent compounds exceeded mevinolin's activity in vitro and in vivo.
MeSH terms
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Animals
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Anticholesteremic Agents
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Carcinoma, Hepatocellular / metabolism
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Chemical Phenomena
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Chemistry
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Cholesterol / biosynthesis*
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Cholesterol / blood
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Dogs
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Heptanoic Acids / chemical synthesis
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Heptanoic Acids / pharmacology*
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Humans
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Hydroxymethylglutaryl-CoA Reductase Inhibitors*
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Liver / drug effects
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Liver / metabolism
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Liver Neoplasms / metabolism
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Lovastatin / pharmacology
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Male
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Molecular Structure
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Pyrroles / chemical synthesis
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Pyrroles / pharmacology*
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Rabbits
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Rats
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Structure-Activity Relationship
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Tumor Cells, Cultured
Substances
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Anticholesteremic Agents
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Heptanoic Acids
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Hydroxymethylglutaryl-CoA Reductase Inhibitors
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Pyrroles
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Cholesterol
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Lovastatin