2. Academic Validation
  3. Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors

Design, synthesis, and pharmacology of novel 7-substituted 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors

  • J Med Chem. 2007 Jun 28;50(13):3153-7. doi: 10.1021/jm070120i.
Pierre Francotte 1,  Pascal de Tullio,  Eric Goffin,  Gaëlle Dintilhac,  Emmanuel Graindorge,  Pierre Fraikin,  Pierre Lestage,  Laurence Danober,  Jean-Yves Thomas,  Daniel-Henri Caignard,  Bernard Pirotte
Affiliations

Affiliation

  • 1 Drug Research Center, Laboratoire de Chimie Pharmaceutique, Université de Liège, Av. de l'Hôpital, 1, B36, 4000 Liège, Belgium. pierre.francotte@ulg.ac.be
PMID: 17552506 DOI: 10.1021/jm070120i
Abstract

A series of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides have been synthesized and evaluated as potentiators of AMPA receptors. Attention was paid to the impact of the substituent introduced at the 7-position of the heterocycle. The biological evaluation was achieved by measuring the AMPA current in rat cortex mRNA-injected Xenopus oocytes. The most potent compound, 4-ethyl-7-fluoro-3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide (12a) was found to be active in an object recognition test in rats demonstrating cognition enhancing effects in vivo after oral administration.

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