Influence of various central moieties on the hypolipidemic properties of long hydrocarbon chain diols and diacids.
J Med Chem
; 49(1): 334-48, 2006 Jan 12.
Article
in En
| MEDLINE
| ID: mdl-16392818
ABSTRACT
A series of long (11-15) hydrocarbon chain diols and diacids with various central functional groups and terminal gem-dimethyl or -methyl/aryl substituents was synthesized and evaluated in both in vivo and in vitro assays for its potential to favorably alter lipid disorders including metabolic syndrome. Compounds were assessed for their effects on the de novo incorporation of radiolabeled acetate into lipids in primary cultures of rat hepatocytes, as well as for their effects on lipid and glycemic variables in obese female Zucker fatty rats, Crl(ZUC)-faBR. The most active compounds were hydroxyl-substituted symmetrical diacids and diols with a 13-atom chain and terminal gem-dimethyl substituents. Furthermore, biological activity was enhanced by central substitution with O, C=O, S, S=O compared to the methylene analogues and was diminished for compounds with central functional groups such as carbamate, ester, urea, acetylmethylene, and hydroxymethylene.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Diabetes Mellitus, Experimental
/
Dicarboxylic Acids
/
Alcohols
/
Hydrocarbons
/
Hyperlipidemias
/
Hypolipidemic Agents
Type of study:
Prognostic_studies
Limits:
Animals
Language:
En
Journal:
J Med Chem
Journal subject:
QUIMICA
Year:
2006
Document type:
Article
Affiliation country:
United States