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Paper(s) concerning Tacrine-Resveratrol-12

1 reference(s) found.
Listing paper details in reverse chronological order.
We are grateful to Keith Bradnam for improvment of this script

Title: Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease
Jerabek J, Uliassi E, Guidotti L, Korabecny J, Soukup O, Sepsova V, Hrabinova M, Kuca K, Bartolini M and Bolognesi ML <4 more author(s)> Jerabek J, Uliassi E, Guidotti L, Korabecny J, Soukup O, Sepsova V, Hrabinova M, Kuca K, Bartolini M, Pena-Altamira LE, Petralla S, Monti B, Roberti M, Bolognesi ML (- 4)
Ref: Eur Journal of Medicinal Chemistry, 127:250, 2016 : PubMed
Abstract


ESTHER: Jerabek_2016_Eur.J.Med.Chem_127_250
PubMedSearch: Jerabek 2016 Eur.J.Med.Chem 127 250
PubMedID: 28064079
Inhibitor(s) related to this paper: Tacrine-Resveratrol-12

Abstract

Multi-target drug discovery is one of the most followed approaches in the active central nervous system (CNS) therapeutic area, especially in the search for new drugs against Alzheimer's disease (AD). This is because innovative multi-target-directed ligands (MTDLs) could more adequately address the complexity of this pathological condition. In a continuation of our efforts aimed at a new series of anti-AD MTDLs, we combined the structural features of the cholinesterase inhibitor drug tacrine with that of resveratrol, which is known for its purported antioxidant and anti-neuroinflammatory activities. The most interesting hybrid compounds (5, 8, 9 and 12) inhibited human acetylcholinesterase at micromolar concentrations and effectively modulated Abeta self-aggregation in vitro. In addition, 12 showed intriguing anti-inflammatory and immuno-modulatory properties in neuronal and glial AD cell models. Importantly, the MTDL profile is accompanied by high-predicted blood-brain barrier permeability, and low cytotoxicity on primary neurons.