Synthesis and potent anticonvulsant activities of 4-oxo-imidazo[1,2-a]indeno[1,2-e]pyrazin-8- and -9-carboxylic (acetic) acid AMPA antagonists
| Autor: | John Randle, Alain Boireau, Jean-Marie Stutzmann, Patrick Jimonet, Jeremy Pratt, Dominique Damour, Arielle Genevois-Borella, Serge Mignani, Marc Williams Debono, Marc Vuilhorgne, Yves Ribeill, Georg Andrees Bohme |
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| Rok vydání: | 2000 |
| Předmět: |
chemistry.chemical_classification
Stereochemistry medicine.medical_treatment Organic Chemistry Clinical Biochemistry Glutamate receptor Pharmaceutical Science AMPA receptor Biochemistry Amino acid Acetic acid chemistry.chemical_compound Anticonvulsant chemistry Drug Discovery medicine Molecular Medicine Antagonism Receptor Molecular Biology Ionotropic effect |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:2749-2754 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)00561-8 |
| Popis: | The over-stimulation of excitatory amino acid receptors such as the glutamate AMPA receptor has been suggested to be associated with neurodegenerative disorders. Here we describe an original series of readily water soluble 4-oxo-imidazo[1,2-a] indeno[1,2-e]pyrazin-8- and -9-carboxylic (acetic) acid derivatives. One of these compounds, 4f, exhibited nanomolar binding affinity, potent competitive antagonism at the ionotropic AMPA receptor and a long duration of anticonvulsant activity after administration by parenteral route in vivo. |
| Databáze: | OpenAIRE |
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