202858-58-0Relevant academic research and scientific papers
Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists
Ladouceur, Gaetan H.,Cook, James H.,Hertzog, Donald L.,Jones,Hundertmark, Thomas,Korpusik, Mary,Lease, Timothy G.,Livingston, James N.,MacDougall, Margit L.,Osterhout, Martin H.,Phelan, Kathleen,Romero, Romulo H.,Schoen, William R.,Shao, Chunning,Smith, Roger A.
, p. 3421 - 3424 (2007/10/03)
Optimized substituent patterns in 4-aryl-pyridine glucagon receptor antagonists were merged to produce highly potent derivatives containing both a 3-[(1R)-hydroxyethyl] and a 2′-hydroxy group. Due to restricted rotation of the phenyl-pyridine bond, these analogues exist as four isomers. A diastereoselective methylcopper reaction was developed to facilitate the synthesis, and single isomers were isolated with activities in the range IC50=10-25 nM.
