Novel heterocyclic glucocorticoids: in vitro profile and in vivo efficacy

A series of novel ligands for the glucocorticoid receptor containing two heterocycles were synthesized. These compounds were investigated for a dissociative profile using transrepression and transactivation assays. Several compounds were tested in vivo and showed the ability to reduce inflammation in a mouse.

Compound 15 displayed the profile of a dissociated glucocorticoid in vitro and reduced inflammation in a mouse.Figure optionsDownload as PowerPoint slide