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Abstract To develop more potent small molecules with enhanced free radical scavenger properties, a series of <it>N</it>-substituted isatin derivatives was synthesized, and the cytoprotective effect on the apoptosis of PC12 cells induced by H2O2 was screened. All these compounds were found to be active, and <it>N</it>-ethyl isatin was found with the most potent activity of 69.7% protective effect on PC12 cells. Structure-activity relationship analyses showed the bioactivity of <it>N</it>-alkyl isatins decline as the increasing of the chain of the alkyl group, furthermore odd-even effect was found in the activity, which is interesting for further investigation.</p

Simple isatin derivatives as free radical scavengers: Synthesis, biological evaluation and structure-activity relationship