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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acetylcholinesterase (AChE) inhibitor and the first approved drug for the treatment of Alzheimer’s disease (AD), was withdrawn from the market due to its side effects, particularly its hepatotoxicity.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

  • Czech description

Classification

  • Type

    J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database

  • CEP classification

  • 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

  • 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