Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists
…, WR Schoen, ML MacDougall, JN Livingston
Index: Ladouceur, Gaetan H.; Cook, James H.; Doherty, Elizabeth M.; Schoen, William R.; MacDougall, Margit L.; Livingston, James N. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 3 p. 461 - 464
Full Text: HTML
Citation Number: 37
Abstract
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, IC50= 0.11 μM, more than 60-fold improvement over the lead structure.
Related Articles:
Zeofen: a user friendly agent for oxidation of the Hantzsch 1, 4-dihydropyridines
[Heravi, Majid M.; Derikvand, Fatemeh; Oskooie, Hossein A.; Hekmatshoar, Rahim Journal of Chemical Research, 2006 , # 3 p. 168 - 169]
[Sharbatdaran, Masoomeh; Foruzin, Leila Jafari; Farzaneh, Faezeh; Larijani, Majid Mojtahedzadeh Comptes Rendus Chimie, 2013 , vol. 16, # 2 p. 176 - 182]
[Nasr-Esfahani, Masoud; Karami, Bahador; Behzadi, Masoume Journal of Heterocyclic Chemistry, 2009 , vol. 46, # 5 p. 931 - 935]
Indium-mediated deoxygenation of amine-N-oxides in aqueous media
[Yadav; Subba Reddy; Reddy, M. Muralidhar Tetrahedron Letters, 2000 , vol. 41, # 15 p. 2663 - 2665]
Rapid, high-yield oxidation of Hantzsch-type 1, 4-dihydropyridines with ceric ammonium nitrate
[Pfister Synthesis, 1990 , # 8 p. 689 - 690]