RT Journal Article
T1 Evaluation of the Antioxidant and Neuroprotectant Activities of New Asymmetrical 1,3-Diketones
A1 Nieto, Carla
A1 Cornago, María
A1 Cabildo, María
A1 Sanz, Dionisia
A1 Claramunt, Rosa
A1 Torralba Martínez, María Del Carmen
A1 Torres, María del Rosario
A1 Martínez Casanova, Diana
A1 Sánchez-Alegre, Yaiza
A1 Escudero, Esther
A1 Lavandera, José
AB A series of fourteen new asymmetrical 1,3-diketone derivatives have been synthesized and evaluated in the ABTS, FRAP and DPPH assays as a new chemotype with antioxidant and drug-like properties. All the compounds displayed low cytotoxicity in comparison to curcumin against the human neuroblastoma SH-SY5Y cell line. Among them, (3Z,5E)-6-(2,5-difluoro-4-hydroxy-phenyl)-1,1,1-trifluoro-4-hydroxyhexa-3,5-dien-2-one (6b) and (3Z,5E)-6-(2,3-difluoro-4-hydroxy-phenyl)-1,1,1-trifluoro-4-hydroxyhexa-3,5-dien-2-one (7b) with excellent solubility and chemical stability in biorelevant media, have also shown a similar Fe+2 chelation behavior to that of curcumin. Additionally, both derivatives 6b and 7b have afforded good neuroprotection activity against H2O2 induced oxidative stress in the same neuronal cell line, with a significant reduction of intracellular ROS levels, in parallel with a good recovery of the Mitochondrial Membrane Potential (ΔΨm). Compounds 6b and 7b with a promising antioxidant and drug-like profile, with low cytotoxic and good neuroprotectant activity, constitute a new interesting chemical class with high potential as new therapeutic agents against neurodegenerative diseases.
PB MDPI
SN 1420-3049
YR 2018
FD 2018-07-24
LK https://hdl.handle.net/20.500.14352/12634
UL https://hdl.handle.net/20.500.14352/12634
LA eng
NO Ministerio de Economía y Competitividad (MINECO)
DS Docta Complutense
RD 10 abr 2025