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Neuroinflammation plays a crucial role in the progression of Alzheimer’s disease and other neurodegenerative disorders. Overactivated microglia cause neurotoxicity and prolong the inflammatory response in many neuropathologies. In this study, we have synthesised a series of isatin derivatives to evaluate their anti-neuroinflammatory potential using lipopolysaccharide activated microglia as a cell model. We explored four different substitutions of the isatin moiety by testing their anti-neuroinflammatory activity on BV2 microglia cells. Based on the low cytotoxicity and the activity in reducing the release of nitric oxide, pro-inflammatory interleukin 6 and tumour necrosis factor α by microglial cells, the <i>N¹</i>-alkylated compound <b>10</b> and the chlorinated <b>20</b> showed the best results at 25 µM. Taken together, the data suggest that <b>10</b> and <b>20</b> are promising lead compounds for developing new neuroprotective agents.