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

• Verfasst von: Meyer, Kirstin [VerfasserIn]
• Verfasst von: Voss, Edgar [VerfasserIn]
• Verfasst von: Neidlein, Richard [VerfasserIn]
• Verfasst von: Kühnle, Hans-Frieder [VerfasserIn]
• Verfasst von: Pill, Johannes [VerfasserIn]
• Titel: ω-substituted alkyl carboxylic acids as antidiabetic and lipid-lowering agents
• Verf.angabe: Kirstin Meyer, Edgar Voss, Richard Neidlein, Hans-Frieder Kühnle, Johannes Pill
• Jahr: 1998
• Umfang: 13 S.
• Fussnoten: Elektronische Reproduktion der Druck-Ausgabe 20. Mai 1999 ; Gesehen am 06.07.2023
• Titel Quelle: Enthalten in: European journal of medicinal chemistry
• Ort Quelle: Amsterdam [u.a.] : Elsevier Science, 1987
• Jahr Quelle: 1998
• Band/Heft Quelle: 33(1998), 10, Seite 775-787
• ISSN Quelle: 1768-3254
• DOI: doi:10.1016/S0223-5234(99)80029-4
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: insulin sensitizer
• Sach-SW: lipid lowering
• Sach-SW: ω-substituted alkyl carboxylic acids
• K10plus-PPN: 1852101113

Abstract

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.