ω-substituted alkyl carboxylic acids as antidiabetic and lipid-lowering agents

In screening experiments certain ω-substituted alkyl carboxylic acids, were found to produce an increase in insulin-stimulated 14C-acetate incorporation into triglycerides, which may indicate an improvement in the action of insulin. Antidiabetic and lipid-lowering properties in genetically diabetic...

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Autores principales: Meyer, Kirstin (Autor) , Voss, Edgar (Autor) , Neidlein, Richard (Autor) , Kühnle, Hans-Frieder (Autor) , Pill, Johannes (Autor)
Formato: Article (Journal)
Lenguaje:inglés
Publicado: 1998
In: European journal of medicinal chemistry
Year: 1998, Volumen: 33, Número: 10, Pages: 775-787
ISSN:1768-3254
DOI:10.1016/S0223-5234(99)80029-4
Acceso en línea:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/S0223-5234(99)80029-4
Verlag, lizenzpflichtig, Volltext: https://www.sciencedirect.com/science/article/pii/S0223523499800294
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Notas de Autor:Kirstin Meyer, Edgar Voss, Richard Neidlein, Hans-Frieder Kühnle, Johannes Pill
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Sumario:In screening experiments certain ω-substituted alkyl carboxylic acids, were found to produce an increase in insulin-stimulated 14C-acetate incorporation into triglycerides, which may indicate an improvement in the action of insulin. Antidiabetic and lipid-lowering properties in genetically diabetic ob/ob mice demonstrated the in vivo relevance of the insulin-potentiating effects seen in vitro. The chemical structures of the ω-substituted alkyl carboxylic acids with insulin-potentiating effects correspond to the general formula ring-spacer-COOH. A close structure-activity relationship was observed. The most potent compound in ob/ob mice was 3e, which normalized blood glucose as well as hyperinsulinaemia and lowered serum triglycerides and cholesterol by 52% and 37%, respectively. On the basis of these results, ω-substituted alkyl carboxylic acids are interesting as a new class of oral antidiabetic agents with insulin-sensitizing and lipid-lowering activity.
Notas:Elektronische Reproduktion der Druck-Ausgabe 20. Mai 1999
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Descripción Física:Online Resource
ISSN:1768-3254
DOI:10.1016/S0223-5234(99)80029-4