Modification of biologically active amides and amines with fluorine-containing heterocycles 12.* Endo- and exocyclic modifications of the drug riluzole with trifluoromethyl-containing heterocycles


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Abstract

New derivatives of the drug riluzole, 6-(trifluoromethoxy)benzothiazol-2-ylamine, modified at the endo- and exocyclic nitrogen atoms with trifluoromethyl-containing heterocycles were synthesized via transformations of methyltrifluoropyruvate and hexafluoroacetone N-6-(trifluoromethoxy)benzothiazol-2-ylimines by meams of cycloaddition and cyclocondensation reactions, respectively. The influence of the resulting compounds on neuronal NMDA receptors, as well as on the release and reuptake of the neurotransmitter glutamate was investigated.

About the authors

V. B. Sokolov

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Author for correspondence.
Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432

A. Yu. Aksinenko

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432

A. V. Sokolov

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432

A. Gabrelian

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432

A. D. Efimova

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432

V. V. Grigoriev

Institute of Physiologically Active Compounds, Russian Academy of Sciences

Email: alaks@ipac.ac.ru
Russian Federation, 1 Severnyi proezd, Chernogolovka, Moscow Region, 142432


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