N-Phenylacetylglycyl-L-Proline Ethyl Ester Converts into Cyclo-L-Prolylglycine Showing a Similar Spectrum of Neuropsychotropic Activity
- 作者: Gudasheva T.1, Kolyasnikova K.1, Kuznetsova E.1, Litvinova S.1, Zolotov N.1, Voronina T.1, Ostrovskaya R.1, Seredenin S.1
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隶属关系:
- V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
- 期: 卷 50, 编号 11 (2017)
- 页面: 705-710
- 栏目: Search for New Drugs
- URL: https://journals.rcsi.science/0091-150X/article/view/244463
- DOI: https://doi.org/10.1007/s11094-017-1516-4
- ID: 244463
如何引用文章
详细
Previously designed cyclo-L-prolylglycine (CPG), a peptide prototype of piracetam, was discovered as an endogenous compound in rat brain and exhibited nootropic and anxiolytic properties. N-Phenylacetylglycyl-L-proline ethyl ester (GZK-111) was synthesized in the present work. It was established that GZK-111 converted to CPG and possessed nootropic, anxiolytic, and antihypoxic activities typical of CPG at doses of 0.1 – 1.5 mg/kg (i.p.). The effects of both GZK-111 and CPG were stereoselective with only the L-enantiomers being active. GZK-111 could be considered as a prodrug that enhanced cognitive functioning with an anxiolytic component.
作者简介
T. Gudasheva
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
K. Kolyasnikova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
E. Kuznetsova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
S. Litvinova
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
N. Zolotov
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
T. Voronina
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
R. Ostrovskaya
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315
S. Seredenin
V. V. Zakusov Institute of Pharmacology, Russian Academy of Medical Sciences
Email: chem@folium.ru
俄罗斯联邦, 8 Baltiiskaya St., Moscow, 125315