Tryptophanol-derived oxazolopiperidone lactams: Identification of a hit compound as NMDA receptor antagonist

Autor:	Pereira, N.A.L., Sureda, F.X., Esplugas, R., Pérez, M., Amat, M., Santos, M.M.M.
Přispěvatelé:	Ciències Mèdiques Bàsiques, Universitat Rovira i Virgili.
Rok vydání:	2014
Předmět:	Sistema nerviós -- degeneració nervous system 0960-894X
Zdroj:	Bioorganic & Medicinal Chemistry Letters Repositori Institucional de la Universitat Rovira i Virgili Universitat Rovira i virgili (URV)
Popis:	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 63.4 µM in cultured rat cerebellar granule neurons thus being 1.5 fold more active than clinically approved NMDA antagonist amantadine (IC50 = 92 µM)
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::3982a358c4956a7ffbe5c6570367c863 http://hdl.handle.net/20.500.11797/PC981 Zobrazit plný text záznamu