7-methoxytacrine-p-anisidine hybrids as novel dual binding site acetylcholinesterase inhibitors for Alzheimer's disease treatment
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F15%3A43914846" target="_blank" >RIV/00023752:_____/15:43914846 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/15:43875524 RIV/00179906:_____/15:10319536
Result on the web
<a href="http://www.mdpi.com/1420-3049/20/12/19836" target="_blank" >http://www.mdpi.com/1420-3049/20/12/19836</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/molecules201219836" target="_blank" >10.3390/molecules201219836</a>
Alternative languages
Result language
angličtina
Original language name
7-methoxytacrine-p-anisidine hybrids as novel dual binding site acetylcholinesterase inhibitors for Alzheimer's disease treatment
Original language description
Alzheimer's disease (AD) is a debilitating progressive neurodegenerative disorder that ultimately leads to the patient's death. Despite the fact that novel pharmacological approaches endeavoring to block the neurodegenerative process are still emerging, none of them have reached use in clinical practice yet. Thus, palliative treatment represented by acetylcholinesterase inhibitors (AChEIs) and memantine are still the only therapeutics used. Following the multi-target directed ligands (MTDLs) strategy, herein we describe the synthesis, biological evaluation and docking studies for novel 7-methoxytacrine-p-anisidine hybrids designed to purposely target both cholinesterases and the amyloid cascade. Indeed, the novel derivatives proved to be effective non-specific cholinesterase inhibitors showing non-competitive AChE inhibition patterns. This compounds' behavior was confirmed in the subsequent molecular modeling studies.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
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Result continuities
Project
<a href="/en/project/GAP303%2F11%2F1907" target="_blank" >GAP303/11/1907: Novel inhibitors of acetylcholinesterase derived from 7-MEOTA - potential Alzheimer´s disease drugs</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Molecules
ISSN
1420-3049
e-ISSN
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Volume of the periodical
20
Issue of the periodical within the volume
12
Country of publishing house
CH - SWITZERLAND
Number of pages
18
Pages from-to
22084-22101
UT code for WoS article
000367533400081
EID of the result in the Scopus database
2-s2.0-84954356941