N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity

The logical framework approach was implemented for designing CNS-active N-substituted 1H-pyrimidin-4-ones. Formation energies of possible ligand—receptor complexes with D2-dopamine and GABAA Receptors were determined from molecular docking calculations. The results allowed the probability of psychot...

Descrición completa

Gardado en:

Detalles Bibliográficos
Главные авторы:	Manvelyan, E. A., Манвелян, Э. А.
Formato:	Статья
Idioma:	English
Publicado:	Springer New York LLC 2018
Темы:	Anxiolytic activity D2-dopamine and GABAA receptors Molecular design Pyrimidin-4-ones Targeted synthesis
Acceso en liña:	https://www.scopus.com/record/display.uri?eid=2-s2.0-85029121020&origin=resultslist&sort=plf-f&src=s&nlo=1&nlr=20&nls=afprfnm-t&affilName=nort+caucas+fed+univ&sid=1946c417b781d61d9cf2ec314093a48c&sot=afnl&sdt=cl&cluster=scopubyr%2c%222017%22%2ct&sl=53&s=%28AF-ID%28%22North+Caucasus+Federal+University%22+60070541%29%29&relpos=37&citeCnt=0&searchTerm= https://dspace.ncfu.ru:443/handle/20.500.12258/692
Метки:	Engadir etiqueta Sen Etiquetas, Sexa o primeiro en etiquetar este rexistro!

id	ir-20.500.12258-692
record_format	dspace
spelling	ir-20.500.12258-6922020-07-30T10:07:06Z N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity Manvelyan, E. A. Манвелян, Э. А. Anxiolytic activity D2-dopamine and GABAA receptors Molecular design Pyrimidin-4-ones Targeted synthesis The logical framework approach was implemented for designing CNS-active N-substituted 1H-pyrimidin-4-ones. Formation energies of possible ligand—receptor complexes with D2-dopamine and GABAA Receptors were determined from molecular docking calculations. The results allowed the probability of psychotropic activity manifesting in the modeled compounds to be estimated. The most promising compounds were prepared by a modified synthetic procedure. The effect of the heteroatom type in N-heterocyclic 1H-pyrimidin-4-ones on the product yield was studied. Compounds I – IV and VI at a dose of 50 mg/kg exhibited anticonflict activity. The mercaptotriazole derivative of pyrimidin-4-one had the greatest anticonflict activity 2018-06-20T14:03:34Z 2018-06-20T14:03:34Z 2017 Статья Oganesyan, É.T., Kodonidi, I.P., Bandura, A.F., Sochnev, V.S., Manvelyan, É.A., Sysa, V.Y. N-Substituted 1H-Pyrimidin-4-One Derivatives Possessing Anxiolytic Activity // Pharmaceutical Chemistry Journal. - 2017. - Volume 51. - Issue 5. - pp. 361-365 https://www.scopus.com/record/display.uri?eid=2-s2.0-85029121020&origin=resultslist&sort=plf-f&src=s&nlo=1&nlr=20&nls=afprfnm-t&affilName=nort+caucas+fed+univ&sid=1946c417b781d61d9cf2ec314093a48c&sot=afnl&sdt=cl&cluster=scopubyr%2c%222017%22%2ct&sl=53&s=%28AF-ID%28%22North+Caucasus+Federal+University%22+60070541%29%29&relpos=37&citeCnt=0&searchTerm= https://dspace.ncfu.ru:443/handle/20.500.12258/692 en Pharmaceutical Chemistry Journal application/pdf application/pdf Springer New York LLC
institution	СКФУ
collection	Репозиторий
language	English
topic	Anxiolytic activity D2-dopamine and GABAA receptors Molecular design Pyrimidin-4-ones Targeted synthesis
spellingShingle	Anxiolytic activity D2-dopamine and GABAA receptors Molecular design Pyrimidin-4-ones Targeted synthesis Manvelyan, E. A. Манвелян, Э. А. N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
description	The logical framework approach was implemented for designing CNS-active N-substituted 1H-pyrimidin-4-ones. Formation energies of possible ligand—receptor complexes with D2-dopamine and GABAA Receptors were determined from molecular docking calculations. The results allowed the probability of psychotropic activity manifesting in the modeled compounds to be estimated. The most promising compounds were prepared by a modified synthetic procedure. The effect of the heteroatom type in N-heterocyclic 1H-pyrimidin-4-ones on the product yield was studied. Compounds I – IV and VI at a dose of 50 mg/kg exhibited anticonflict activity. The mercaptotriazole derivative of pyrimidin-4-one had the greatest anticonflict activity
format	Статья
author	Manvelyan, E. A. Манвелян, Э. А.
author_facet	Manvelyan, E. A. Манвелян, Э. А.
author_sort	Manvelyan, E. A.
title	N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
title_short	N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
title_full	N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
title_fullStr	N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
title_full_unstemmed	N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity
title_sort	n-substituted 1h-pyrimidin-4-one derivatives possessing anxiolytic activity
publisher	Springer New York LLC
publishDate	2018
url	https://www.scopus.com/record/display.uri?eid=2-s2.0-85029121020&origin=resultslist&sort=plf-f&src=s&nlo=1&nlr=20&nls=afprfnm-t&affilName=nort+caucas+fed+univ&sid=1946c417b781d61d9cf2ec314093a48c&sot=afnl&sdt=cl&cluster=scopubyr%2c%222017%22%2ct&sl=53&s=%28AF-ID%28%22North+Caucasus+Federal+University%22+60070541%29%29&relpos=37&citeCnt=0&searchTerm= https://dspace.ncfu.ru:443/handle/20.500.12258/692
work_keys_str_mv	AT manvelyanea nsubstituted1hpyrimidin4onederivativespossessinganxiolyticactivity AT manvelânéa nsubstituted1hpyrimidin4onederivativespossessinganxiolyticactivity
_version_	1760600882447122432

N-substituted 1H-pyrimidin-4-one derivatives possessing anxiolytic activity

Títulos similares