Optimization of triarylimidazoles for Tie2: Influence of conformation on potency

In an effort to understand the effect of N-alkylation of triarylimidazoles on Tie2 inhibition, ortho-substituted C-2 aryl analogs were synthesized to investigate the effect of different torsion angles on potency. This exercise resulted in the identification of a potent and selective tetrasubstituted imidazole that was efficacious in an animal model of angiogenesis.

Optimization of triarylimidazoles for Tie2 potency resulted in the identification of the potent and selective tetrasubstituted imidazole 23 that was efficacious in an animal model of angiogenesis.Figure optionsDownload as PowerPoint slide