Document Detail


Hypolipidemic activity of a series of N-pyridinyl and N-quinolinyl substituted derivatives of phthalimide and succinimides in rodents.
MedLine Citation:
PMID:  2360899     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
N-Pyridinyl- and N-quinolinyl-ethyl substituted succinimide and phthalimide derivatives demonstrated significant hypolipidemic activity in rodents lowering both serum cholesterol and triglyceride levels at 20 mg/kg.day i.p. The pyridinyl, quinolinyl and tetrahydro-2-quinolinyl substitution improved the hypolipidemic activity of the succinimide derivatives. Whereas select N-quinolinylethylphthalimide derivatives demonstrated less activity than phthalimide, itself, in lowering serum cholesterol and triglyceride levels, they did cause significant increases in HDL cholesterol and lower LDL cholesterol levels after 14 days of drug administration. Phthalimide actually caused reductions of HDL cholesterol levels in rats. These new agents with heterocyclic substitution of the N atom of phthalimide increased fecal excretion of lipids and suppressed in vitro hepatic rate limiting enzyme activities for de novo synthesis of cholesterol, fatty acids and triglycerides. Acute toxicity studies of the N-quinolinylethylphthalimide derivatives indicated that the agents are safe as potential therapeutic agents at doses necessary for hypolipidemic activity.
Authors:
I H Hall; O T Wong; G Futch; J P Scovill
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Biomedica biochimica acta     Volume:  49     ISSN:  0232-766X     ISO Abbreviation:  Biomed. Biochim. Acta     Publication Date:  1990  
Date Detail:
Created Date:  1990-08-01     Completed Date:  1990-08-01     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  8304435     Medline TA:  Biomed Biochim Acta     Country:  GERMANY, EAST    
Other Details:
Languages:  eng     Pagination:  103-13     Citation Subset:  IM    
Affiliation:
Division of Medicinal Chemistry & Natural Products, School of Pharmacy, University of North Carolina, Chapel Hill 27599.
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MeSH Terms
Descriptor/Qualifier:
Animals
Aorta / drug effects,  metabolism
Chemical Phenomena
Chemistry
Cholesterol, HDL / deficiency*,  metabolism
Feces / analysis
Intestine, Small / drug effects,  metabolism
Isoquinolines / pharmacology
Liver / drug effects,  metabolism*
Male
Mice
Phthalimides / pharmacology*
Rats
Rats, Inbred Strains
Succinimides / pharmacology*
Chemical
Reg. No./Substance:
0/Cholesterol, HDL; 0/Isoquinolines; 0/Phthalimides; 0/Succinimides; 119-65-3/isoquinoline

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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