Hypolipidemic activity of substituted 2-pyrrolidinones in rodents
✍ Scribed by George H. Cocolas; James M. Chapman Jr.; P. Josée Voorstad; Iris H. Hall
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- English
- Weight
- 329 KB
- Volume
- 72
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
A series of substituted 2-pyrrolidinones was evaluated for hypolipidemic activity a t 20 and 30 mg/kg/day in CF1 male mice. 4-Phenyl-5,5-dicarbethoxy-2-pyrrolidinone was the most potent compound a t 30 mg/kg/day, reducing serum triglyceride levels 52% after 14 days of dosing and serum cholesterol levels 48% after 16 days of dosing. 4-Phenyl-5-carbethoxy-2-pyrrolidinone and 4-phenyl-3,5,5-tricarbethoxy-2-pyrrolidinone also demonstrated significant activity. Those compounds which contained a phenyl substituent were more potent than either the unsubstituted, the alkyl, or the dicarbethoxy 2-pyrrolidinone analogues.
Keyphrases 0 2-Pyrrolidinones-synthesis of substituted analogues, hypolipidemic activity in mice 0 Antihyperlipidemic agentssubstituted 2-pyrrolidinone analogues, synthesis, hypolipidemic activity in mice Succinimide-2-pyrrolidinone congeners, synthesis of substituted analogues, hypolipidemic activity in mice ' Fisher, Hycel Triglyceride Test (1975). Hycel. Inc.
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Previously, a series of N-substituted indazolone derivatives proved to be effective hypolipidemic agents in rodents. The most effective agent, N2-n-butylindazolone, at 20 mg/kg/d was shown to suppress the levels of cytoplasm acetyl coenzyme A required for cholesterol and fatty acid synthesis as well