КФУ. Карточка публикации. Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase

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MACROCYCLIC DERIVATIVES OF 6-METHYLURACIL AS LIGANDS OF THE PERIPHERAL ANIONIC SITE OF ACETYLCHOLINESTERASE

Форма представления

Статьи в зарубежных журналах и сборниках

Год публикации

2014

Авторы, сотрудники КФУ

Зобов Владимир Васильевич, автор

Библиографическое описание на языке оригинала

Semenov, V.E. Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase / V.E. Semenov, R.Kh. Giniyatullin, S.V. Lushchekina, E.D. Kots, K.A. Petrov, A.D. Nikitashina, O.A. Minnekhanova, V.V. Zobov, E.E. Nikolsky, P. Masson, V.S. Reznik // MedChemComm. -2014, V. 5, Issue 11, -P. 1729-1735

Аннотация

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

Ключевые слова

макроциклы, урацилы, ацетилхолинэстераза

Название журнала

Med. Chem. Commun.

URL

http://pubs.rsc.org/en/content/articlelanding/2014/md/c4md00225c#!divAbstract

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https://repository.kpfu.ru/?p_id=91845

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Полная запись метаданных

Поле DC	Значение	Язык
dc.contributor.author	Зобов Владимир Васильевич	ru_RU
dc.date.accessioned	2014-01-01T00:00:00Z	ru_RU
dc.date.available	2014-01-01T00:00:00Z	ru_RU
dc.date.issued	2014	ru_RU
dc.identifier.citation	Semenov, V.E. Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase / V.E. Semenov, R.Kh. Giniyatullin, S.V. Lushchekina, E.D. Kots, K.A. Petrov, A.D. Nikitashina, O.A. Minnekhanova, V.V. Zobov, E.E. Nikolsky, P. Masson, V.S. Reznik // MedChemComm. -2014, V. 5, Issue 11, -P. 1729-1735	ru_RU
dc.identifier.uri	https://repository.kpfu.ru/?p_id=91845	ru_RU
dc.description.abstract	Med. Chem. Commun.	ru_RU
dc.description.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	ru_RU
dc.language.iso	ru	ru_RU
dc.subject	макроциклы	ru_RU
dc.subject	урацилы	ru_RU
dc.subject	ацетилхолинэстераза	ru_RU
dc.title	Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase	ru_RU
dc.type	Статьи в зарубежных журналах и сборниках	ru_RU