Modification of biologically active amides and amines by fluoro-containing heterocycles 10. γ-Carbolines modified by 2-trifluoromethylimidazo-[1,2-a]pyridin-3-ylpropionamide fragments

被引:8
作者
Bachurin, S. O. [1 ]
Sokolov, V. B. [1 ]
Aksinenko, A. Yu. [1 ]
Epishina, T. A. [1 ]
Goreva, T. V. [1 ]
Grigor'ev, V. V. [1 ]
Zamoiskii, V. L. [1 ]
Gabrel'yan, A. V. [1 ]
机构
[1] Russian Acad Sci, Inst Physiologically Act Cpds, Chernogolovka 142432, Moscow Region, Russia
基金
俄罗斯基础研究基金会;
关键词
gamma-carbolines; substituted 2-trifluoromethylimidazo[1,2-a]pyridines; 3-(1,2,3,4-tetrahydro-5H-pyrido[4,3-b] indol-5-yl)-N-methyl-N-[2-(trifluoromethyl)imidazo[1,2-a]-pyridin-3-yl] propanamides; radioligand binding; COGNITION; DIMEBON;
D O I
10.1007/s11172-013-0352-2
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An approach to the modification of biologically active gamma-carbolines by the 2-trifluoromethyl-imidazo[1,2-a] pyridin-3-ylpropionamide fragments was suggested, which consisted of the reaction of N-methyl-N-(2-trifluoromethylimidazo[1,2-a] pyridin-3-yl) prop-2-enamides with gamma-carbolines in the presence of catalytic amounts of cesium fluoride. Method of radioligand binding was used to study effects of the synthesized 3-(1,2,3,4-tetrahydro-5H-pyrido[4,3-b]-indol-5-yl)-N-methyl-N-[2-(trifluoromethyl) imidazo-[1,2-a] pyridin-3-yl] propanamides on the neuronal NMDA-receptors.
引用
收藏
页码:2438 / 2441
页数:4
相关论文
共 16 条
  • [1] Modification of gamma-carbolines with N-substituted propionamides as a new approach to mitoprotective agents
    Bachurin, S. O.
    Vinogradova, D. V.
    Shevtsova, E. F.
    Goreva, T. V.
    Epishina, T. A.
    Aksinenko, A. Yu.
    Sokolov, V. B.
    [J]. RUSSIAN CHEMICAL BULLETIN, 2013, 62 (03) : 816 - 819
  • [2] Hindering of proteinopathy-induced neurodegeneration as a new mechanism of action for neuroprotectors and cognition enhancing compounds
    Bachurin, S. O.
    Ustyugov, A. A.
    Peters, O.
    Shelkovnikova, T. A.
    Buchman, V. L.
    Ninkina, N. N.
    [J]. DOKLADY BIOCHEMISTRY AND BIOPHYSICS, 2009, 428 (01) : 235 - 238
  • [3] Bachurin S. O., 2010, VESTNIK RAN, V80, p[497, 80]
  • [4] Bachurin S. O., Pat. RF, Patent No. 2490268
  • [5] Bachurin S. O., 2001, NEIRODEGENERATIVNYE, P399
  • [6] PHARMACOLOGICAL CHARACTERIZATION AND AUTORADIOGRAPHIC DISTRIBUTION OF POLYAMINE-SENSITIVE [H-3] IFENPRODIL BINDING-SITES IN THE RAT-BRAIN
    DANA, C
    BENAVIDES, J
    SCHOEMAKER, H
    SCATTON, B
    [J]. NEUROSCIENCE LETTERS, 1991, 125 (01) : 45 - 48
  • [7] Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study
    Doody, Rachelle S.
    Gavrilova, Svetlana I.
    Sano, Mary
    Thomas, Ronald G.
    Aisen, Paul S.
    Bachurin, Sergey O.
    Seely, Lynn
    Hung, David
    [J]. LANCET, 2008, 372 (9634) : 207 - 215
  • [8] Modern approaches to the design of memory and cognitive enhancers based on AMPA receptor ligands
    Grigoriev, V. V.
    Proshin, A. N.
    Kinzirsky, A. S.
    Bachurin, S. O.
    [J]. RUSSIAN CHEMICAL REVIEWS, 2009, 78 (05) : 485 - 494
  • [9] KOCHETKOV N, 1961, ZH OBSHCH KHIM+, V31, P924
  • [10] Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential
    Mony, Laetitia
    Kew, James N. C.
    Gunthorpe, Martin J.
    Paoletti, Pierre
    [J]. BRITISH JOURNAL OF PHARMACOLOGY, 2009, 157 (08) : 1301 - 1317