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

Abstract : Antioxidant 8-alkylamino-1,4-benzoxazines, (R,S)-(3-tert-butyl-8-phenylethylamino-3,4-dihydro-2H-1,4-benzoxazin-5-yl) (phenyl) methanone (S 24429) and (R,S)-(3-cyclopentyl-8-benzylamino-3,4-dihydro-2H-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 mg 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.
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Submitted on : Friday, November 12, 2010 - 10:44:47 AM
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Martine Largeron, Bettina Mesples, Pierre Gressens, Roméo Cecchelli, Michael Spedding, et al.. The neuroprotective activity of 8-alkylamino-1, 4-benzoxazine antioxidants. European Journal of Pharmacology, Elsevier, 2001, 424, p. 189-194. ⟨hal-00535639⟩

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