| Abstract
| - A series of new 8-amino-1,4-benzoxazine derivatives 5a−o was synthesized and examined fortheir intrinsic cytotoxicity and their capacity to inhibit oxidative stress-mediated neuronaldegeneration in neuronal cell cultures. In particular, substituent effects at the 3- and 8-positionsof the 1,4-benzoxazine ring were investigated by in vitro evaluation. In this aim, 3-alkylsubstituents seemed to be essential for efficient neuroprotective activity. Furthermore, withinthe subseries of substituted 3-alkyl benzoxazines, the most active derivatives were those bearingan 8-benzylamino substituent. From the combined results of both toxicity and neuroprotectionexpressed in terms of the safety index, 8-benzylamino-substituted-3-alkyl-1,4-benzoxazines wereidentified as the most promising compounds, owing to their potent neuroprotective activitywithout the manifestation of intrinsic cytotoxicity.
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