(+/-)-BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3 beta Inhibition with Calcium Channel Antagonism and Antiaggregating Properties for Alzheimer's Disease

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F21%3A10428687" target="_blank" >RIV/00179906:_____/21:10428687 - isvavai.cz</a>
Alternative codes found
RIV/62690094:18470/21:50018074 RIV/60162694:G44__/21:00556982
Result on the web
<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=yxs8WYdo6Y" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=yxs8WYdo6Y</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acschemneuro.0c00803" target="_blank" >10.1021/acschemneuro.0c00803</a>

Result language
angličtina
Original language name
(+/-)-BIGI-3h: Pentatarget-Directed Ligand combining Cholinesterase, Monoamine Oxidase, and Glycogen Synthase Kinase 3 beta Inhibition with Calcium Channel Antagonism and Antiaggregating Properties for Alzheimer's Disease
Original language description
Multitarget-directed ligands (MTDLs) are considered a promising therapeutic strategy to address the multifactorial nature of Alzheimer's disease (AD). Novel MTDLs have been designed as inhibitors of human acetylcholinesterases/ butyrylcholinesterases, monoamine oxidase A/B, and glycogen synthase kinase 3 beta and as calcium channel antagonists via the Biginelli multicomponent reaction. Among these MTDLs, (+/-)-BIGI-3h was identified as a promising new hit compound showing in vitro balanced activities toward the aforementioned recognized AD targets. Additional in vitro studies demonstrated antioxidant effects and brain penetration, along with the ability to inhibit the aggregation of both t protein and beta-amyloid peptide. The in vivo studies have shown that (+/-)-BIGI-3h (10 mg/kg intraperitoneally) significantly reduces scopolamine-induced cognitive deficits.
Czech name
—
Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy

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
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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