Synthesis and Anticonvulsant Activity of New 2-(4-Oxo-2-Thioxo-1,4-Dihydro-3(2h)-Quinazolinyl)Acetamides
Bunyatyan N. D., Severina H. I., Mokhamad E. K. W., Zalevskyi S. V., Shtrygol’ S. Y., Shark A. A., Tsyvunin V. V., Kompantsev D. V., Shevchenko A. M., Kovalenko S. N., Georgiyants V. A., Ogay M. A., Khadzhieva Z. J.
Pharmaceutical Chemistry Journal
Опубликовано: 2020
Тип ресурса: Статья
DOI:10.1007/s11094-020-02147-5
Аннотация:
A search for new anticonvulsants led to a series of 2-(4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)- acetamides that were synthesized by reacting (4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)acetic acid with the appropriate amines in the presence of N,N′-carbonyldiimidazole. The tested compounds showed weak and moderate anticonvulsant effects in a pentylenetetrazole-induced seizure model in mice. Several features of the structure—activity relationships are discussed. © 2020, Springer Science+Business Media, LLC, part of Springer Nature.
Ключевые слова:
acetamides; anticonvulsants; quinazoline; synthesis
acetamide derivative; anticonvulsive agent; new drug; valproic acid; animal experiment; animal model; anticonvulsant activity; Article; controlled study; drug synthesis; female; latent period; liquid chromatography-mass spectrometry; male; melting point; mouse; nonhuman; pentylenetetrazole-induced convulsion; structure activity relation; substitution reaction; thin layer chromatography; tonic seizure
Язык текста: Английский
ISSN: 1573-9031
Bunyatyan N. D. Natal`ya Dmitrievna 1955-
Severina H. I.
Mokhamad E. K. W.
Zalevskyi S. V.
Shtrygol’ S. Y.
Shark A. A.
Tsyvunin V. V.
Kompantsev D. V.
Shevchenko A. M.
Kovalenko S. N. Sergej Nikolaevich 1959-
Georgiyants V. A.
Ogay M. A.
Khadzhieva Z. J.
Бунятян Н. Д. Наталья Дмитриевна 1955-
Северина Х. И.
Мохамад Е. К. W.
Залевскyи С. В.
Штрyгол’ С. Y.
Шарк А. А.
Цyвунин В. В.
Компанцев Д. В.
Шевченко А. М.
Коваленко С. Н. Сергей Николаевич 1959-
Георгиянц В. А.
Огай М. А.
Хаджиева З. Й.
Synthesis and Anticonvulsant Activity of New 2-(4-Oxo-2-Thioxo-1,4-Dihydro-3(2h)-Quinazolinyl)Acetamides
Текст визуальный непосредственный
Pharmaceutical Chemistry Journal
Springer New York Consultants Bureau
Vol.54, Issue1
2020
Статья
acetamides anticonvulsants quinazoline synthesis
acetamide derivative anticonvulsive agent new drug valproic acid animal experiment animal model anticonvulsant activity Article controlled study drug synthesis female latent period liquid chromatography-mass spectrometry male melting point mouse nonhuman pentylenetetrazole-induced convulsion structure activity relation substitution reaction thin layer chromatography tonic seizure
A search for new anticonvulsants led to a series of 2-(4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)- acetamides that were synthesized by reacting (4-oxo-2-thioxo-1,4-dihydro-3(2H)-quinazolinyl)acetic acid with the appropriate amines in the presence of N,N′-carbonyldiimidazole. The tested compounds showed weak and moderate anticonvulsant effects in a pentylenetetrazole-induced seizure model in mice. Several features of the structure—activity relationships are discussed. © 2020, Springer Science+Business Media, LLC, part of Springer Nature.