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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Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 1990-01, Vol.33 (1), p.61-70
Hauptverfasser:	Jendralla, H, Baader, E, Bartmann, W, Beck, G, Bergmann, A, Granzer, E, Von Kerekjarto, B, Kesseler, K, Krause, R
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00163a011