Cenalmor Molina, AlejandroPascual Vega, ElenaGil-Manso, SergioCorrea-Rocha, RafaelSuárez Álvarez, José RamónGarcía-Álvarez, Isabel2024-02-092024-02-092023Cenalmor A, Pascual E, Gil-Manso S, Correa-Rocha R, Suárez JR, García-Álvarez I. Evaluation of Anti-Neuroinflammatory Activity of Isatin Derivatives in Activated Microglia. Molecules 2023;28:4882. https://doi.org/10.3390/molecules28124882.1420-304910.3390/molecules28124882https://hdl.handle.net/20.500.14352/100868Neuroinflammation 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 N1-alkylated compound 10 and the chlorinated 20 showed the best results at 25 µM. Taken together, the data suggest that 10 and 20 are promising lead compounds for developing new neuroprotective agents.engAttribution 4.0 Internationalhttp://creativecommons.org/licenses/by/4.0/journal articlehttps://doi.org/10.3390/molecules28124882https://www.mdpi.com/1420-3049/28/12/4882open access615:54615.31NeuroinflammationMicrogliaIsatinNitric oxideInterleukin 6TNF-αCiencias Biomédicas23 Química