A series of Glucocorticoid Receptor(GR) ligands utilizing imidazo[4,5-b]pyrazine isosteres for acylaminothiadiazoles in the azaxanthene series is reported.  These partial agonists (2-27) retain not only high GR affinity and selectivity (e.g., over progesterone receptor), but also display an improved pharmacokinetic profile over the lead thiadiazole amide (compound 1). SAR and general methods for synthesis are described.

Imidazo[4,5-b]pyrazines as thiadiazole amide isosteres in the 5H-chromeno[2,3-b]pyridine (azaxanthene) series of glucocorticoid receptor(GR) agonists

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.