Synthesis of 4-Phenylpyrrolidone Derivatives with Anticonvulsant and Nootropic Activity
- Авторы: Zhmurenko L.A.1, Litvinova S.A.1, Mokrov G.V.1, Kovalev I.G.1, Voronina T.A.1, Nerobkova L.N.1, Gudasheva T.A.1
- 
							Учреждения: 
							- V. V. Zakusov Research Institute of Pharmacology
 
- Выпуск: Том 53, № 5 (2019)
- Страницы: 429-435
- Раздел: Article
- URL: https://ogarev-online.ru/0091-150X/article/view/245797
- DOI: https://doi.org/10.1007/s11094-019-02015-x
- ID: 245797
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Аннотация
New 4-phenylpyrrolidone derivatives were designed from racetam structures that combine nootropic and anticonvulsant activity. The proposed compounds were synthesized using 4-phenylpyrrolidone and aromatic amines. The anticonvulsant activity of the new compounds was studied. The structure–activity relationship was analyzed. The most active compound was the 2,6-dimethylanilide of (2-oxo-4-phenylpyrrolidin-1-yl)acetic acid at doses of 2.5 – 5.0 mg/kg, which surpassed the reference drug levetiracetam at doses of 2.5 – 600 mg/kg in all tests and possessed distinct nootropic activity that was comparable to that of the reference nootropic drug piracetam at a dose of 400 mg/kg.
Об авторах
L. Zhmurenko
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
S. Litvinova
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
G. Mokrov
V. V. Zakusov Research Institute of Pharmacology
							Автор, ответственный за переписку.
							Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
I. Kovalev
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
T. Voronina
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
L. Nerobkova
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
T. Gudasheva
V. V. Zakusov Research Institute of Pharmacology
														Email: g.mokrov@gmail.com
				                					                																			                												                	Россия, 							8 Baltiiskaya St., Moscow, 125315						
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