7-Methoxytacrine-Adamantylamine Heterodimers as Cholinesterase Inhibitors in Alzheimer's Disease Treatment - Synthesis, Biological Evaluation and Molecular Modeling Studies

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F13%3A10133341" target="_blank" >RIV/00179906:_____/13:10133341 - isvavai.cz</a>

Alternative codes found

RIV/60162694:G44__/13:43874768 RIV/00216208:11160/13:10133341

Result on the web

<a href="http://www.mdpi.com/1420-3049/18/2/2397" target="_blank" >http://www.mdpi.com/1420-3049/18/2/2397</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules18022397" target="_blank" >10.3390/molecules18022397</a>

Result language

angličtina

Original language name

7-Methoxytacrine-Adamantylamine Heterodimers as Cholinesterase Inhibitors in Alzheimer's Disease Treatment - Synthesis, Biological Evaluation and Molecular Modeling Studies

Original language description

A structural series of 7-MEOTA-adamantylamine thioureas was designed, synthesized and evaluated as inhibitors of human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE). The compounds were prepared based on the multi-target-directed ligand strategy with different linker lengths (n = 2-8) joining the well-known NMDA antagonist adamantine and the hAChE inhibitor 7-methoxytacrine (7-MEOTA). Based on in silico studies, these inhibitors proved dual binding site character capable of simultaneous interaction with the peripheral anionic site (PAS) of hAChE and the catalytic active site (CAS). Clearly, these structural derivatives exhibited very good inhibitory activity towards hBChE resulting in more selective inhibitors of this enzyme. Themost potent cholinesterase inhibitor was found to be thiourea analogue 14 (with an IC50 value of 0.47 mu M for hAChE and an IC50 value of 0.11 mu M for hBChE, respectively). Molecule 14 is a suitable novel lead compound for further evalua

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

Result was created during the realization of more than one project. More information in the Projects tab.

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2013

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Molecules

ISSN

1420-3049

e-ISSN

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Volume of the periodical

18

Issue of the periodical within the volume

2

Country of publishing house

CH - SWITZERLAND

Number of pages

22

Pages from-to

2397-2418

UT code for WoS article

000315400600078

EID of the result in the Scopus database

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