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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| Main Authors: | , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
1998
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| In: |
European journal of medicinal chemistry
Year: 1998, Volume: 33, Issue: 10, Pages: 775-787 |
| ISSN: | 1768-3254 |
| DOI: | 10.1016/S0223-5234(99)80029-4 |
| Online Access: | 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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| Author Notes: | Kirstin Meyer, Edgar Voss, Richard Neidlein, Hans-Frieder Kühnle, Johannes Pill |
| Summary: | 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. |
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| Item Description: | Elektronische Reproduktion der Druck-Ausgabe 20. Mai 1999 Gesehen am 06.07.2023 |
| Physical Description: | Online Resource |
| ISSN: | 1768-3254 |
| DOI: | 10.1016/S0223-5234(99)80029-4 |