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Título: | Optimization of Bicyclic Lactam Derivatives as NMDA Receptor Antagonists |
Autor: | Espadinha, M.; Dourado, J; Lajarín-Cuesta, Rocío; Herrera-Arozamena, Clara CSIC ORCID CVN; Gonçalves, Lidia M. D.; Rodríguez-Franco, María Isabel CSIC ORCID ; Ríos, Cristobal de los; Santos, María M. M. | Palabras clave: | Antagonists Nitrogen heterocycles NMDA receptors Bicyclic lactams Asymmetric synthesis |
Fecha de publicación: | 2017 | Editor: | Wiley-VCH | Citación: | ChemMedChem 12: 537-545 (2017) | Resumen: | N-Methyl-d-aspartate (NMDA) receptors are fundamental for the normal function of the central nervous system (CNS), and play an important role in memory and learning. Over-activation of these receptors leads to neuronal loss associated with major neurological disorders such as Parkinson's disease, Alzheimer's disease, schizophrenia, and epilepsy. In this study, 22 novel enantiopure bicyclic lactams were designed, synthesized, and evaluated as NMDA receptor antagonists. Most of the new compounds displayed NMDA receptor antagonism, and the most promising compound showed an IC value on the same order of magnitude as that of memantine, an NMDA receptor antagonist in clinical use for the treatment of Alzheimer's disease. Further biological evaluation indicated that this compound is brain permeable (determined by an in vitro assay) and non-hepatotoxic. All these results indicate that (3S,7aS)-7a-(4-chlorophenyl)-3-(4-hydroxybenzyl)tetrahydropyrrolo[2,1-b]oxazol-5(6H)-one (compound 5 b) is a potential candidate for the treatment of pathologies associated with the over-activation of NMDA receptors. | Versión del editor: | http://dx.doi.org/10.1002/cmdc.201700037 | URI: | http://hdl.handle.net/10261/149788 | DOI: | 10.1002/cmdc.201700037 | Identificadores: | doi: 10.1002/cmdc.201700037 issn: 1860-7187 e-issn: 1860-7187 |
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Optimization of bicyclic lactam.pdf | 755,12 kB | Adobe PDF | Visualizar/Abrir |
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