Synthesis and biological evaluations of condensed pyridine and condensed pyrimidine-based HMG-CoA reductase inhibitors.
Bioorg Med Chem Lett
; 11(10): 1285-8, 2001 May 21.
Article
de En
| MEDLINE
| ID: mdl-11392538
ABSTRACT
A series of 3,5-dihydroxyheptenoic acid derivatives containing pyrazolopyridine, isoxazolopyridine, thienopyridine, and pyrazolopyrimidine as a key scaffold was synthesized from condensed pyridine and condensed pyrimidine carboxylic acid esters by homologation, aldol condensation with ethyl acetoacetate dianion, and stereoselective reduction of the 5-hydroxyketone. Several compounds in the series were found to have potent HMG-CoA reductase inhibitory activities in vitro and marked cholesterol biosynthesis inhibitory activities in vivo. It has been shown that these scaffolds can be used as a suitable replacement for the hexahydronaphthalene ring present in naturally occurring HMG-CoA reductase inhibitors.
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Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Pyridines
/
Pyrimidines
/
Inhibiteurs de l'hydroxyméthylglutaryl-CoA réductase
Limites:
Animals
/
Humans
/
Male
Langue:
En
Journal:
Bioorg Med Chem Lett
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2001
Type de document:
Article
Pays d'affiliation:
Japon