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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists.

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 IC(50)=10-25 nM.[1]

References

  1. Integration of optimized substituent patterns to produce highly potent 4-aryl-pyridine glucagon receptor antagonists. Ladouceur, G.H., Cook, J.H., Hertzog, D.L., Jones, J.H., Hundertmark, T., Korpusik, M., Lease, T.G., Livingston, J.N., MacDougall, M.L., Osterhout, M.H., Phelan, K., Romero, R.H., Schoen, W.R., Shao, C., Smith, R.A. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
 
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