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JOURNALS // Mendeleev Communications // Archive

Mendeleev Commun., 2023 Volume 33, Issue 1, Pages 70–72 (Mi mendc311)

This article is cited in 5 papers

Communications

New 1,11-dimethyl-3,6,9-triazatricyclo[7.3.1.13,11]tetradecane-4,8,12-trione derivative as an allosteric modulator of the glutamatergic system

E. A. Golubevaa, M. I. Lavrova, P. N. Veremeevaa, E. M. Bovinaa, E. V. Radchenkoa, M. A. Topchiyb, A. F. Asachenkob, V. L. Zamoyskic, V. V. Grigorievac, V. A. Palyulina

a Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow, Russian Federation
b A.V. Topchiev Institute of Petrochemical Synthesis, Russian Academy of Sciences, Moscow, Russian Federation
c Institute of Physiologically Active Compounds, Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, Russian Academy of Sciences, Chernogolovka, Moscow Region, Russian Federation

Abstract: An optimized synthesis of N-{5-[(1,11-dimethyl-4,8,12-trioxo-3,6,9-triazatricyclo[7.3.1.13,11]tetradec-6-yl)methyl]-indan-2-yl}-1,3-benzodioxole-5-carboxamide has been carried out from indan-2-one oxime in seven steps. In vitro studies using electrophysiological patch clamp technique have revealed a positive modulation effect of this compound on kainate induced currents in Purkinje neurons in a wide range of concentrations from 10–12 to 10–8 m.

Keywords: 3,7-diazabicyclo[3.3.1]nonanes, indane derivatives, piperonylic acid, cross-coupling, nitriles, AMPA receptor, allosteric modulators, PAMs, patch clamp.

Language: English

DOI: 10.1016/j.mencom.2023.01.022



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