Details

Autor(en) / Beteiligte

• Largeron, Martine
• Mesples, Bettina
• Gressens, Pierre
• Cecchelli, Romeo
• Spedding, Michael
• Le Ridant, Alain
• Fleury, Maurice-Bernard

Titel

The neuroprotective activity of 8-alkylamino-1,4-benzoxazine antioxidants

Ist Teil von

• European journal of pharmacology, 2001-07, Vol.424 (3), p.189-194

Ort / Verlag

Amsterdam: Elsevier B.V

Erscheinungsjahr

2001

Link zum Volltext

Quelle

Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)

Beschreibungen/Notizen

• Antioxidant 8-alkylamino-1,4-benzoxazines, ( R, S)-(3- tert-butyl-8-phenylethylamino-3,4-dihydro-2 H-1,4-benzoxazin-5-yl) (phenyl) methanone (S 24429) and ( R, S)-(3-cyclopentyl-8-benzylamino-3,4-dihydro-2 H-1,4-benzoxazin-5-yl) (phenyl) methanone (S 24718), were prepared according to a two-step one-pot electrochemical procedure. These compounds had been selected from a previous study of structure/activity. Both compounds (1–100 μM) prevented the fall in ATP levels caused by 24 h of hypoxia in astrocytes. Both compounds (1 and 10 mg/kg i.p.) were powerful neuroprotective agents in protecting against the lesions induced by 15 μg S-bromo-willardiine injected into the cortex or white matter of 5-day old mice pups. In contrast, exifone, an antioxidant compound, was inactive at these doses. S 24429 and S 24718 appear to be novel neuroprotective agents, which are effective in a model of brain damage mimicking the lesions underlying cerebral palsy.