Discovery of 5-Hydroxyalkyl-4-phenylpyridines as a New Class of Glucagon Receptor Antagonists
5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2002-02, Vol.12 (3), p.461-464 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | 5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery of a potent antagonist, IC
50=0.11 μM, more than 60-fold improvement over the lead structure.
5-Hydroxyalkyl-4-phenylpyridines have been identified as a novel class of glucagon antagonists with potential utility for the treatment of diabetes. A lead structure with moderate activity was discovered through a high throughput screening assay. Structure–activity relationships led to the discovery of a potent antagonist. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/S0960-894X(01)00766-1 |