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.
Jendralla
H
H
Hoechst AG, Frankfurt (Main), West Germany.
Baader
E
E
Bartmann
W
W
Beck
G
G
Bergmann
A
A
Granzer
E
E
von Kerekjarto
B
B
Kesseler
K
K
Krause
R
R
Schubert
W
W
D000818:Animals; D000924:Anticholesteremic Agents; D006528:Carcinoma, Hepatocellular / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D002784:Cholesterol / Q000096:biosynthesis* / Q000097:blood; D004285:Dogs; D006538:Heptanoic Acids / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D008099:Liver / Q000187:drug effects / Q000378:metabolism; D008113:Liver Neoplasms / Q000378:metabolism; D008148:Lovastatin / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis / Q000494:pharmacology*; D011817:Rabbits; D051381:Rats; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000924:Anticholesteremic Agents; D006538:Heptanoic Acids; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D011758:Pyrroles; D002784:Cholesterol; D008148:Lovastatin