Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors - implications for early Myasthenia gravis treatment
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F11%3A10100523" target="_blank" >RIV/00216208:11160/11:10100523 - isvavai.cz</a>
Alternative codes found
RIV/60162694:G44__/11:00002426 RIV/44555601:13440/11:43881362
Result on the web
<a href="http://www.sciencedirect.com/science/article/pii/S0960894X11002319" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0960894X11002319</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmcl.2011.02.047" target="_blank" >10.1016/j.bmcl.2011.02.047</a>
Alternative languages
Result language
angličtina
Original language name
Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors - implications for early Myasthenia gravis treatment
Original language description
This paper describes the preparation and in vitro evaluation of 18 newly prepared bis-quinolinium inhibitors on human recombinant acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase (BChE). Their inhibitory (IC(50)) and was compared tothe chosen standards ambenonium dichloride, edrophonium chloride, BW284c51 and ethopropazine hydrochloride. One novel compound was found to be a promising inhibitor of hAChE (in nM range) and was better than edrophonium chloride or BW284c51, but was worse than ambenonium chloride. This compound also showed selectivity towards hAChE and it was confirmed as a non-competitive inhibitor of hAChE by kinetic analysis. A molecular modelling study further confirmed its binding to the peripheral active site of hAChE via apparent pi-pi or pi-cationic interactions.
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/GP203%2F09%2FP130" target="_blank" >GP203/09/P130: Development of novel acetylcholinesterase inhibitors as treatment of Myasthenia Gravis</a><br>
Continuities
S - Specificky vyzkum na vysokych skolach
Others
Publication year
2011
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Bioorganic and Medicinal Chemistry Letters
ISSN
0960-894X
e-ISSN
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Volume of the periodical
21
Issue of the periodical within the volume
8
Country of publishing house
GB - UNITED KINGDOM
Number of pages
5
Pages from-to
2505-2509
UT code for WoS article
000289074700070
EID of the result in the Scopus database
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