A novel class of allosteric modulators of AMPA/Kainate receptors

The rapid hydrolysis in vivo of IDRA21 to 2-amino-5-chlorobenzensulfonamide has been demonstrated by microdialysis experiments. The IDRA21 metabolite possess in vitro a biological activity similar to that of IDRA21 itself. Taking 2-amino-5-chlorobenzensulfonamide as lead compound, a novel class of AMPAR positive allosteric modulators has been prepared.

IDRA21 is one of the most potent cognitive enhancers. We have demonstrated that in vivo IDRA21 (1) was quickly hydrolyzed to 2-amino-5-chlobenzensulfonamide that posses in vitro a biological activity similar to that of IDRA21 itself. Taking 2-amino-5-chlobenzensulfonamide as the lead compound, a novel class of AMPAR positive allosteric modulators has been prepared.Figure optionsDownload as PowerPoint slide