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.
A novel class of allosteric modulators of AMPA/Kainate receptors / Cannazza, G., Krzysztof, J., Parenti, C., Braghiroli, D., Carrozzo, M.M., Puja, G., Losi, G., Baraldi, M., Wolfgang, L., Irving W., W.. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 19:4(2009), pp. 1254-1257. [10.1016/j.bmcl.2008.12.094]
A novel class of allosteric modulators of AMPA/Kainate receptors
CANNAZZA, Giuseppe;PARENTI, Carlo;BRAGHIROLI, Daniela;CARROZZO, Marina Maria;PUJA, Giulia;LOSI, Gabriele;BARALDI, Mario;
2009
Abstract
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.
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