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 ML; Cavalli A; Bergamini C; Fato R; Lenaz G; Rosini M; Bartolini M; Andrisano V; Melchiorre C.. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - STAMPA. - 52:(2009), pp. 7883-7886. [10.1021/jm901123n]
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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
