Development of 2-methoxyhuprine as novel lead for Alzheimer’s disease therapy
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00023752%3A_____%2F17%3A43919282" target="_blank" >RIV/00023752:_____/17:43919282 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/17:43889182 RIV/62690094:18470/17:50013430 RIV/00216208:11160/17:10362378 RIV/00179906:_____/17:10362378
Result on the web
<a href="http://www.mdpi.com/1420-3049/22/8/1265" target="_blank" >http://www.mdpi.com/1420-3049/22/8/1265</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/molecules22081265" target="_blank" >10.3390/molecules22081265</a>
Alternative languages
Result language
angličtina
Original language name
Development of 2-methoxyhuprine as novel lead for Alzheimer’s disease therapy
Original language description
Tacrine (THA), the first clinically effective acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer’s disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity. Nowadays, THA serves as a valuable scaffold for the design of novel agents potentially applicable for AD treatment. One such compound, namely 7-methoxytacrine (7-MEOTA), exhibits an intriguing profile, having suppressed hepatotoxicity and concomitantly retaining AChE inhibition properties. Another interesting class of AChE inhibitors represents Huprines, designed by merging two fragments of the known AChE inhibitors—THA and (−)-huperzine A. Several members of this compound family are more potent human AChE inhibitors than the parent compounds. The most promising are so-called huprines X and Y. Here, we report the design, synthesis, biological evaluation, and in silico studies of 2-methoxyhuprine that amalgamates structural features of 7-MEOTA and huprine Y in one molecule.
Czech name
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Czech description
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Classification
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
10401 - Organic chemistry
Result continuities
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)
Others
Publication year
2017
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
22
Issue of the periodical within the volume
8
Country of publishing house
CH - SWITZERLAND
Number of pages
19
Pages from-to
"Article Number: 1265"
UT code for WoS article
000408602900030
EID of the result in the Scopus database
2-s2.0-85028344296