3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors: oxime ether analogs of pravastatin. 1995

N Turabi, and R A DiPietro, and S Mantha, and C Ciosek, and L Rich, and J I Tu
Diagnostics Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA.

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.

UI MeSH Term Description Entries
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000924 Anticholesteremic Agents Substances used to lower plasma CHOLESTEROL levels. Cholesterol Inhibitors,Hypocholesteremic Agents,Anticholesteremic Drugs,Anticholesteremics,Inhibitors, Cholesterol,Agents, Anticholesteremic,Agents, Hypocholesteremic,Drugs, Anticholesteremic
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D017035 Pravastatin An antilipemic fungal metabolite isolated from cultures of Nocardia autotrophica. It acts as a competitive inhibitor of HMG CoA reductase (HYDROXYMETHYLGLUTARYL COA REDUCTASES). Eptastatin,Apo-Pravastatin,Bristacol,CS-514,Elisor,Lin-Pravastatin,Lipemol,Liplat,Lipostat,Mevalotin,Nu-Pravastatin,Prareduct,Pravachol,Pravacol,Pravasin,Pravastatin Monosodium Salt, (6 beta)-Isomer,Pravastatin Sodium,Pravastatin Sodium Salt,Pravastatin tert-Octylamine Salt,Pravastatin, (6 beta)-Isomer,RMS-431,SQ-31,000,SQ-31000,Selektine,Vasten,Apo Pravastatin,CS 514,CS514,Lin Pravastatin,Nu Pravastatin,Pravastatin tert Octylamine Salt,RMS 431,RMS431,SQ 31,000,SQ 31000,SQ31,000,SQ31000,Sodium Salt, Pravastatin
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D019161 Hydroxymethylglutaryl-CoA Reductase Inhibitors Compounds that inhibit HYDROXYMETHYLGLUTARYL COA REDUCTASES. They have been shown to directly lower CHOLESTEROL synthesis. HMG-CoA Reductase Inhibitor,HMG-CoA Reductase Inhibitors,Hydroxymethylglutaryl-CoA Reductase Inhibitor,Statin,Statins, HMG-CoA,Inhibitors, HMG-CoA Reductase,Inhibitors, Hydroxymethylglutaryl-CoA,Inhibitors, Hydroxymethylglutaryl-Coenzyme A,Statins,HMG CoA Reductase Inhibitor,HMG CoA Reductase Inhibitors,HMG-CoA Statins,Hydroxymethylglutaryl CoA Reductase Inhibitor,Hydroxymethylglutaryl CoA Reductase Inhibitors,Hydroxymethylglutaryl-CoA Inhibitors,Hydroxymethylglutaryl-Coenzyme A Inhibitors,Inhibitors, HMG CoA Reductase,Inhibitors, Hydroxymethylglutaryl CoA,Inhibitors, Hydroxymethylglutaryl Coenzyme A,Inhibitors, Hydroxymethylglutaryl-CoA Reductase,Reductase Inhibitor, Hydroxymethylglutaryl-CoA,Reductase Inhibitors, HMG-CoA,Reductase Inhibitors, Hydroxymethylglutaryl-CoA,Statins, HMG CoA

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