Design of potent and selective GSK3β inhibitors with acceptable safety profile and pharmacokinetics

From potent and selective inhibitors of GSK3β displaying CYP1A2 inhibition and poor PK properties, mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives.

Graphical abstractFrom potent and selective inhibitors of GSK3β displaying CYP1A2 inhibition and poor PK properties mostly linked to metabolic instability and in vivo hydrolysis of the amide bond, we were able to obtain safe and orally available inhibitors with good half lives.Figure optionsDownload full-size imageDownload as PowerPoint slide