Literature DB >> 22197388

6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.

David Orain1, Silvio Ofner, Manuel Koller, David A Carcache, Wolfgang Froestl, Hans Allgeier, Vittorio Rasetti, Joachim Nozulak, Henri Mattes, Nicolas Soldermann, Philipp Floersheim, Sandrine Desrayaud, Joerg Kallen, Kurt Lingenhoehl, Stephan Urwyler.   

Abstract

A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage.
Copyright © 2011. Published by Elsevier Ltd.

Entities:  

Mesh：

Substances：

Year:  2011        PMID： 22197388     DOI： 10.1016/j.bmcl.2011.12.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Ionic liquid versus prodrug strategy to address formulation challenges.

Authors:  Anja Balk; Toni Widmer; Johannes Wiest; Heike Bruhn; Jens-Christoph Rybak; Philipp Matthes; Klaus Müller-Buschbaum; Anastasios Sakalis; Tessa Lühmann; Jörg Berghausen; Ulrike Holzgrabe; Bruno Galli; Lorenz Meinel
Journal:  Pharm Res       Date:  2014-12-23       Impact factor: 4.200

2.  Discovery of Quinazoline-2,4(1H,3H)-Dione Derivatives as Potential Antibacterial Agent: Design, Synthesis, and Their Antibacterial Activity.

Authors:  Nader M Boshta; Farag A El-Essawy; Mohammed B Alshammari; Safaa G Noreldein; Osama M Darwesh
Journal:  Molecules       Date:  2022-06-15       Impact factor: 4.927

Review 3.  AMPA receptors as a molecular target in epilepsy therapy.

Authors:  M A Rogawski
Journal:  Acta Neurol Scand Suppl       Date:  2013

4.  Structure and organization of heteromeric AMPA-type glutamate receptors.

Authors:  Beatriz Herguedas; Javier García-Nafría; Ondrej Cais; Rafael Fernández-Leiro; James Krieger; Hinze Ho; Ingo H Greger
Journal:  Science       Date:  2016-03-10       Impact factor: 47.728

5.  Antitarget Interaction, Acute Toxicity and Protein Binding Studies of Quinazolinedione Sulphonamides as GABA1 Antagonists.

Authors:  Mansi Verma; Sangeeta Rani; A Kumar
Journal:  Indian J Pharm Sci       Date:  2016 Jan-Feb       Impact factor: 0.975
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.