Journal of Medicinal Chemistry · 1990 · 64 citations · 0 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryEnzymologyStructure-activity RelationshipsEnzyme InhibitionStructure-activity Relationship AnalysisBiological Activity FeaturesChemical Synthesis Of AnaloguesHmg-coa Lyase ActivityHmg-coa Reductase InhibitorsMedicinal Chemistry ApplicationsSubstituent Effects On Biological Activity
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.