Synthesis and biological activity of new HMG-CoA reductase inhibitors. 2. Derivatives of 7-(1H-pyrrol-3-yl)-substituted-3,5-dihydroxyhept-6(E)-enoic (-heptanoic) acids

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.

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 33; no. 1; pp. 61 - 70
Main Authors Jendralla, H, Baader, E, Bartmann, W, Beck, G, Bergmann, A, Granzer, E, Von Kerekjarto, B, Kesseler, K, Krause, R
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.01.1990
Subjects
Animals
Anticholesteremic Agents
Carcinoma, Hepatocellular - metabolism
Chemical Phenomena
Chemistry
Cholesterol - biosynthesis
Cholesterol - blood
Dogs
Heptanoic Acids - chemical synthesis
Heptanoic Acids - pharmacology
Humans
Hydroxymethylglutaryl-CoA Reductase Inhibitors
Liver - drug effects
Liver - metabolism
Liver Neoplasms - metabolism
Lovastatin - pharmacology
Male
Molecular Structure
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Rabbits
Rats
Structure-Activity Relationship
Tumor Cells, Cultured
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Summary: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.
Bibliography:istex:F52BD91FC7E25349438BE3C4C764190E2AD45EBB
ark:/67375/TPS-H6JRHBZ6-G
ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00163a011