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Novel acetylcholinesterase inhibitors based on uracil moiety for possible treatment of Alzheimer disease

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dc.contributor.author Semenov V.E.
dc.contributor.author Zueva I.V.
dc.contributor.author Mukhamedyarov M.A.
dc.contributor.author Lushchekina S.V.
dc.contributor.author Petukhova E.O.
dc.contributor.author Gubaidullina L.M.
dc.contributor.author Krylova E.S.
dc.contributor.author Saifina L.F.
dc.contributor.author Lenina O.A.
dc.contributor.author Petrov K.A.
dc.date.accessioned 2021-02-25T20:56:11Z
dc.date.available 2021-02-25T20:56:11Z
dc.date.issued 2020
dc.identifier.uri https://dspace.kpfu.ru/xmlui/handle/net/162714
dc.description.abstract © 2020 by the authors In this study, novel derivatives based on 6-methyluracil and condensed uracil were synthesized, namely, 2,4-quinazoline-2,4-dione with ω-(ortho-nitrilebenzylethylamino) alkyl chains at the N atoms of the pyrimidine ring. In this series of synthesized compounds, the polymethylene chains were varied from having tetra- to hexamethylene chains, and secondary NH, tertiary ethylamino, and quaternary ammonium groups were introduced into the chains. The molecular modeling of the compounds indicated that they could function as dual binding site acetylcholinesterase inhibitors, binding to both the peripheral anionic site and active site. The data from in vitro experiments show that the most active compounds exhibit affinity toward acetylcholinesterase within a nanomolar range, with selectivity for acetylcholinesterase over butyrylcholinesterase reaching four orders of magnitude. In vivo biological assays demonstrated the potency of these compounds in the treatment of memory impairment using an animal model of Alzheimer disease.
dc.subject 6-methyluracil
dc.subject Acetylcholinesterase
dc.subject Alzheimer disease
dc.subject Inhibitors
dc.subject Peripheral anionic site
dc.title Novel acetylcholinesterase inhibitors based on uracil moiety for possible treatment of Alzheimer disease
dc.type Article
dc.relation.ispartofseries-issue 18
dc.relation.ispartofseries-volume 25
dc.collection Публикации сотрудников КФУ
dc.source.id SCOPUS-2020-25-18-SID85090823536


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  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

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