Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase
Vyacheslav Semenov
1
,
Rashit Kh Giniyatullin
1
,
S. Lushchekina
2
,
Ekaterina D. Kots
3
,
Konstantin A Petrov
1, 4, 5
,
Alexandra D Nikitashina
1, 4, 5
,
Oksana A Minnekhanova
1
,
Vladimir V Zobov
1, 5
,
Evgeny E. Nikolsky
1, 4, 5, 6
,
P. Masson
5, 7
,
Vladimir S. Reznik
1
7
DYNAMOP, Institut de Biologie Structurale, Grenoble 38000, France
|
Publication type: Journal Article
Publication date: 2014-09-18
SJR: —
CiteScore: —
Impact factor: —
ISSN: 20402503, 20402511
Organic Chemistry
Drug Discovery
Biochemistry
Pharmacology
Pharmaceutical Science
Molecular Medicine
Abstract
Novel pyrimidinophanes possessing two o-nitrobenzylethyldialkylammonium heads bridging with different spacers were prepared. Pyrimidinophanes 2a, 2b and 3 are reversible inhibitors of cholinesterases. They show a very good selectivity for human acetylcholinesterase (AChE), with an inhibitory power 100–200 times higher than for human butyrylcholinesterase (BChE). Docking simulations indicate specific binding of pyrimidinophanes 2a and 4 onto the peripheral anionic site of AChE. Other compounds bind to the active center of AChE as well as to the peripheral anionic site. These compounds are dual binding site inhibitors. Pyrimidinophane 2b and its acyclic counterpart 1 were tested in the animal model of myasthenia gravis and may be considered as valuable candidates for the treatment of pathological muscle weakness syndromes.
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GOST
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Semenov V. et al. Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase // MedChemComm. 2014. Vol. 5. No. 11. pp. 1729-1735.
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Semenov V., Giniyatullin R. Kh., Lushchekina S., Kots E., Petrov K. A., Nikitashina A. D., Minnekhanova O. A., Zobov V. V., Nikolsky E., Masson P., Reznik V. Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase // MedChemComm. 2014. Vol. 5. No. 11. pp. 1729-1735.
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RIS
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TY - JOUR
DO - 10.1039/C4MD00225C
UR - https://doi.org/10.1039/C4MD00225C
TI - Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase
T2 - MedChemComm
AU - Semenov, Vyacheslav
AU - Giniyatullin, Rashit Kh
AU - Lushchekina, S.
AU - Kots, Ekaterina D.
AU - Petrov, Konstantin A
AU - Nikitashina, Alexandra D
AU - Minnekhanova, Oksana A
AU - Zobov, Vladimir V
AU - Nikolsky, Evgeny E.
AU - Masson, P.
AU - Reznik, Vladimir S.
PY - 2014
DA - 2014/09/18
PB - Royal Society of Chemistry (RSC)
SP - 1729-1735
IS - 11
VL - 5
SN - 2040-2503
SN - 2040-2511
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2014_Semenov,
author = {Vyacheslav Semenov and Rashit Kh Giniyatullin and S. Lushchekina and Ekaterina D. Kots and Konstantin A Petrov and Alexandra D Nikitashina and Oksana A Minnekhanova and Vladimir V Zobov and Evgeny E. Nikolsky and P. Masson and Vladimir S. Reznik},
title = {Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase},
journal = {MedChemComm},
year = {2014},
volume = {5},
publisher = {Royal Society of Chemistry (RSC)},
month = {sep},
url = {https://doi.org/10.1039/C4MD00225C},
number = {11},
pages = {1729--1735},
doi = {10.1039/C4MD00225C}
}
Cite this
MLA
Copy
Semenov, Vyacheslav, et al. “Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase.” MedChemComm, vol. 5, no. 11, Sep. 2014, pp. 1729-1735. https://doi.org/10.1039/C4MD00225C.
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