Novel multitargeted antioxidants 3-6 were designed by combining the antioxidant features, namely, a benzoquinone fragment and a lipoyl function, of two multifunctional lead candidates. They were then evaluated to determine their profile against Alzheimer's disease. They showed antioxidant activity, improved following enzymatic reduction, in mitochondria and T67 cell line. They also displayed a balanced inhibitory profile against amyloid-beta aggregation and acetylcholinesterase, emerging as promising molecules for neuroprotectant lead discovery.

Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks

BOLOGNESI, MARIA LAURA;CAVALLI, ANDREA;BERGAMINI, CHRISTIAN;FATO, ROMANA;LENAZ, GIORGIO;ROSINI, MICHELA;BARTOLINI, MANUELA;ANDRISANO, VINCENZA;MELCHIORRE, CARLO
2009

Abstract

Novel multitargeted antioxidants 3-6 were designed by combining the antioxidant features, namely, a benzoquinone fragment and a lipoyl function, of two multifunctional lead candidates. They were then evaluated to determine their profile against Alzheimer's disease. They showed antioxidant activity, improved following enzymatic reduction, in mitochondria and T67 cell line. They also displayed a balanced inhibitory profile against amyloid-beta aggregation and acetylcholinesterase, emerging as promising molecules for neuroprotectant lead discovery.
JOURNAL OF MEDICINAL CHEMISTRY
Bolognesi ML; Cavalli A; Bergamini C; Fato R; Lenaz G; Rosini M; Bartolini M; Andrisano V; Melchiorre C.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11585/84134
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