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Combined Strategies for the Discovery of Ionotropic Glutamate Receptor Antagonists
Article first published online: 6 MAY 2009
DOI: 10.1002/cmdc.200900109
Copyright © 2009 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Additional Information
How to Cite
Chimirri, A., De Luca, L., Ferro, S., De Sarro, G., Ciranna, L. and Gitto, R. (2009), Combined Strategies for the Discovery of Ionotropic Glutamate Receptor Antagonists. ChemMedChem, 4: 917–922. doi: 10.1002/cmdc.200900109
Publication History
- Issue published online: 28 MAY 2009
- Article first published online: 6 MAY 2009
- Manuscript Revised: 7 APR 2009
- Manuscript Received: 16 MAR 2009
Funded by
- MiUR
- Abstract
- Article
- References
- Cited By
Keywords:
- AMPA;
- antagonists;
- molecular modeling;
- NR2B/NMDA;
- receptors
Abstract
New glutamate receptor ligands: This review describes the discovery of rationally designed AMPA and NMDA receptor antagonists, some of which have been proven to be highly potent anticonvulsant and neuroprotective agents.
This review summarizes the results of our research group engaged in the development of new glutamate receptor ligands. Chemical and biological studies of several active molecules have been carried out. In particular, extensive work has addressed the identification of antagonists of AMPA and NMDA receptor subtypes using a combination of computational strategies. Innovative synthetic pathways have been used and small libraries of new molecules prepared. In vitro and in vivo tests were performed, and some compounds proved to be highly potent anticonvulsant and neuroprotective agents.