334932-35-3Relevant academic research and scientific papers
Discovery of 5-Hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists
Ladouceur, Gaetan H.,Cook, James H.,Doherty, Elizabeth M.,Schoen, William R.,MacDougall, Margit L.,Livingston, James N.
, p. 461 - 464 (2007/10/03)
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.
Substituted biphenyls
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, (2008/06/13)
Substituted biphenyls having glucagon receptor antagonistic activity. Claimed compounds have the formula wherein R1aand R1bindependently represent (C1-C6) alkyl; R2represents (C1-C10) alkyl or substituted (C1-C10) alkyl wherein the substituents are independently from 1 to 3 of —SR7; R7represents phenyl, or substituted phenyl wherein the substituents are independently 1-5 of halogen, trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, nitro, cyano, or hydroxyl; R3represents substituted (C1-C6) alkyl wherein the substituents are 1-2 hydroxyl groups; G represents a substituent selected from the group consisting of halogen, (C1-C6) alkyl, and OR4wherein R4is H or (C1-C6) alkyl; and y is 0 or an integer of 1-3. Pharmaceutical compositions containing such compounds and methods of treatment of glucagon-mediated conditions by administering such compounds are also claimed.
