Document Detail

Tryptophanol-derived oxazolopiperidone lactams: Identification of a hit compound as NMDA receptor antagonist.
MedLine Citation:
PMID:  24974339     Owner:  NLM     Status:  In-Data-Review    
N-Methyl-d-aspartate receptors (NMDAR) exacerbated activation leads to neuron death through a phenomenon called excitotoxicity. These receptors are implicated in several neurological diseases (e.g., Alzheimer and Parkinson) and thus represent an important therapeutic target. We herein describe the study of enantiopure tryptophanol-derived oxazolopiperidone lactams as NMDA receptor antagonists. The most active hit exhibited an IC50 of 63.4μM in cultured rat cerebellar granule neurons thus being 1.5 fold more active than clinically approved NMDA antagonist amantadine (IC50=92μM).
Nuno A L Pereira; Francesc X Sureda; Roser Esplugas; Maria Pérez; Mercedes Amat; Maria M M Santos
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Publication Detail:
Type:  Journal Article     Date:  2014-06-11
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  24     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2014 Aug 
Date Detail:
Created Date:  2014-07-11     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  3333-6     Citation Subset:  IM    
Copyright Information:
Copyright © 2014 Elsevier Ltd. All rights reserved.
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