Analysis of the structural and mechanistic factors in antioxidants that preserve mitochondrial function and confer cytoprotection

作者：Arce Pablo M; Goldschmidt Ruth; Khdour Omar M; Madathil Manikandadas M; Jaruvangsanti Jennifer; Dey Sriloy; Fash David M; Armstrong Jeffrey S; Hecht Sidney M^*

来源：Bioorganic & Medicinal Chemistry, 2012, 20(17): 5188-5201.

DOI：10.1016/j.bmc.2012.07.005

• Idebenone
• Mitochondrial dysfunction
• Reactive oxygen species
• Electron transport chain

Selected pyridinol analogues of the experimental neuroprotective drug idebenone have been synthesized and evaluated as antioxidants capable of preserving mitochondrial function. The compounds, having a different redox core but the same side chain as idebenone, exhibited a range of potencies, reflecting differences in their structures. The results obtained provide guidance in the design of such analogues with improved properties. Analogues were identified that have significantly improved antioxidant activity compared with idebenone in cultured lymphocytes, and which exhibit lesser inhibition of the electron transport chain.

• 出版日期2012-9-1