title: 3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: oxime ether analogs of pravastatin.
abstract: Pravastatin, a potent anti-hypercholesteremic drug, has been developed by Bristol-Myers Squibb for treatment of hypercholesterolemia and other related diseases. Several structurally related compounds (SQ 31,554, SQ 31,879, SQ 31,947, SQ 32,391, SQ 32,770, SQ 32,390 and SQ 32,469) modified at the 3-position of the hexahydronaphthalene ring system of pravastatin were prepared in the course of developing the basic reagents for a radioimmunoassay of the parent drug. The biological activity of these analogs was comparable to pravastatin itself. Indeed, one member of this series was found to be several times more potent than pravastatin.
authors.affiliation: Diagnostics Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA.
authors.forename: N
authors.initials: N
authors.lastname: Turabi
authors.forename: R A
authors.initials: RA
authors.lastname: DiPietro
authors.forename: S
authors.initials: S
authors.lastname: Mantha
authors.forename: C
authors.initials: C
authors.lastname: Ciosek
authors.forename: L
authors.initials: L
authors.lastname: Rich
authors.forename: J I
authors.initials: JI
authors.lastname: Tu
mesh_terms: D000818:Animals; D000924:Anticholesteremic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D017035:Pravastatin / Q000031:analogs & derivatives*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000924:Anticholesteremic Agents; D004791:Enzyme Inhibitors; D019161:Hydroxymethylglutaryl-CoA Reductase Inhibitors; D017035:Pravastatin