Design, synthesis and in vitro testing of 7-methoxytacrine-amantadine analogues: a novel cholinesterase inhibitors for the treatment of Alzheimer's disease
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18450%2F15%3A50003738" target="_blank" >RIV/62690094:18450/15:50003738 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/15:43875388 RIV/00023752:_____/15:43914744 RIV/00179906:_____/15:10295281
Result on the web
<a href="http://link.springer.com/article/10.1007/s00044-015-1316-x/fulltext.html" target="_blank" >http://link.springer.com/article/10.1007/s00044-015-1316-x/fulltext.html</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1007/s00044-015-1316-x" target="_blank" >10.1007/s00044-015-1316-x</a>
Alternative languages
Result language
angličtina
Original language name
Design, synthesis and in vitro testing of 7-methoxytacrine-amantadine analogues: a novel cholinesterase inhibitors for the treatment of Alzheimer's disease
Original language description
A series of cholinesterase inhibitors acting as dual binding site heterodimers for the management of Alzheimer's disease were developed. The series of 7-methoxytacrine (7-MEOTA)-amantadine ureas (11-17) was designed, prepared evaluated in vitro towards human acetyl/butyryl cholinesterase (hAChE, hBChE) and compared with the series of 7-MEOTA-amantadine thioureas (4-10). The heterodimers have different length of linkers combining 7-MEOTA and amantadine moieties. In comparison with 7-MEOTA, the newly synthesized compounds were better inhibitors of both cholinesterases. The urea analogues did not have the anticipated benefit of increased inhibitory activity and have comparable IC50 values with thiourea derivatives.
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
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
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
Medicinal chemistry research
ISSN
1054-2523
e-ISSN
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Volume of the periodical
24
Issue of the periodical within the volume
6
Country of publishing house
US - UNITED STATES
Number of pages
11
Pages from-to
2645-2655
UT code for WoS article
000355933000031
EID of the result in the Scopus database
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