Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F17%3A43915308" target="_blank" >RIV/00023752:_____/17:43915308 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/17:43875734 RIV/00216208:11160/17:10368075 RIV/00179906:_____/17:10368075
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S0223523416310546" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0223523416310546</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.ejmech.2016.12.048" target="_blank" >10.1016/j.ejmech.2016.12.048</a>

Result language
angličtina
Original language name
Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease
Original language description
Multi-target drug discovery is one of the most followed approaches in the active central nervous systém (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 Ab self-aggregation in vitro. In addition, 12 showed intriguing antiinflammatory 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.
Czech name
—
Czech description
—

Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
—
OECD FORD branch
10608 - Biochemistry and molecular biology

Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Similar results(10)