Аннотация:
Molecular modeling, synthesis, and activity evaluation of a novel positive allosteric modulator of the AMPA receptor, 6-[4-methoxy-3-(1H-pyrazol-1-ylmethyl)benzyl]-1,11-dimethyl-3,6,9-triazatricyclo[7.3.1.13,11]tetradecane-4,8,12-trione, are presented. The main point of the design was to fill the interdomain cavity of GluA2 ligand binding domains based on the cyclothiazide binding mode. Electrophysiological studies showed high potentiation of the kainate-induced currents (pECmax∼12).
Тип публикации:
Статья
Язык публикации: английский
Образец цитирования:
M. I. Lavrov, D. S. Karlov, V. A. Palyulin, V. V. Grigoriev, V. L. Zamoyski, G. E. Brkich, N. V. Pyatigorskaya, M. E. Zapolskiy, “Novel positive allosteric modulator of AMPA-receptors based on tricyclic scaffold”, Mendeleev Commun., 28:3 (2018), 311–313
Образцы ссылок на эту страницу:
https://www.mathnet.ru/rus/mendc1749
https://www.mathnet.ru/rus/mendc/v28/i3/p311
Эта публикация цитируется в следующих 16 статьяx:
Sergey A. Pisarev, Elena A. Golubeva, Vladimir A. Palyulin, “Ab Initio Conformational Analysis of 3,7-Diacetyl-3,7-Diazabicyclo[3.3.1]Nonanes”, Natural Product Communications, 19:3 (2024)
Aleksei V. Medved'ko, Savelii V. Gaisen, Mikhail A. Kalinin, Sergey Z. Vatsadze, “Bispidine-Based Macrocycles: Achievements and Perspectives”, Organics, 4:3 (2023), 417
Elena A. Golubeva, Mstislav I. Lavrov, Polina N. Veremeeva, Tatiana V. Vyunova, Konstantin V. Shevchenko, Maxim A. Topchiy, Andrey F. Asachenko, Vladimir A. Palyulin, “New Allosteric Modulators of AMPA Receptors: Synthesis and Study of Their Functional Activity by Radioligand-Receptor Binding Analysis”, IJMS, 24:12 (2023), 10293
E. A. Golubeva, M. I. Lavrov, P. N. Veremeeva, E. M. Bovina, E. V. Radchenko, M. A. Topchiy, A. F. Asachenko, V. L. Zamoyski, V. V. Grigoriev, V. A. Palyulin, “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”, Mendeleev Commun., 33:1 (2023), 70–72
Elena A. Golubeva, Mstislav I. Lavrov, Eugene V. Radchenko, Vladimir A. Palyulin, “Diversity of AMPA Receptor Ligands: Chemotypes, Binding Modes, Mechanisms of Action, and Therapeutic Effects”, Biomolecules, 13:1 (2022), 56
Kseniya N. Sedenkova, Denis V. Zverev, Anna A. Nazarova, Mstislav I. Lavrov, Eugene V. Radchenko, Yuri K. Grishin, Alexey V. Gabrel'yan, Vladimir L. Zamoyski, Vladimir V. Grigoriev, Elena B. Averina, Vladimir A. Palyulin, “Novel Nanomolar Allosteric Modulators of AMPA Receptor of Bis(pyrimidine) Series: Synthesis, Biotesting and SAR Analysis”, Molecules, 27:23 (2022), 8252
M. I. Lavrov, P. N. Veremeeva, E. A. Golubeva, E. V. Radchenko, V. L. Zamoyski, V. V. Grigoriev, V. A. Palyulin, “Positive and negative AMPA receptor modulators based on tricyclic bispidine derivative: Minor structural change inverts the type of activity”, Mendeleev Commun., 32:3 (2022), 360–363
Dmitry A. Vasilenko, Kirill S. Sadovnikov, Kseniya N. Sedenkova, Dmitry S. Karlov, Eugene V. Radchenko, Yuri K. Grishin, Victor B. Rybakov, Tamara S. Kuznetsova, Vladimir L. Zamoyski, Vladimir V. Grigoriev, Vladimir A. Palyulin, Elena B. Averina, “A Facile Approach to Bis(isoxazoles), Promising Ligands of the AMPA Receptor”, Molecules, 26:21 (2021), 6411
E.V. Radchenko, A.S. Tarakanova, D.S. Karlov, M.I. Lavrov, V.A. Palyulin, “Ligands of the AMPA-subtype glutamate receptors: mechanisms of action and novel chemotypes”, BIOMED KHIM, 67:3 (2021), 187
И. Ю. Титов, В. С. Стройлов, П. В. Русина, И. В. Свитанько, “Предварительное моделирование как первая стадия направленного органического синтеза”, Усп. хим., 90:7 (2021), 831–867; I. Yu. Titov, V. S. Stroylov, P. V. Rusina, I. Svitanko, “Preliminary modelling as the first stage of targeted organic synthesis”, Russian Chem. Reviews, 90:7 (2021), 831–867
N. S. Temnyakova, D. A. Vasilenko, M. I. Lavrov, D. S. Karlov, Yu. K. Grishin, V. L. Zamoyski, V. V. Grigoriev, E. B. Averina, V. A. Palyulin, “Novel bivalent positive allosteric AMPA receptor modulator of bis-amide series”, Mendeleev Commun., 31:2 (2021), 216–218
G.E. Brkich, N.V. Pyatigorskaya, V.V. Beregovykh, O.A. Zyryanov, N.B. Demina, E.O. Bakrushina, “The development of the physicochemical characteristics of the new original nootropic substance TST-9”, BIOMED KHIM, 66:3 (2020), 257
P. V. Rusina, I. Yu. Titov, M. V. Panova, V. S. Stroylov, Ya. R. Abdyusheva, E. Yu. Murlatova, I. Svitanko, F. N. Novikov, “Modeling of novel CDK7 inhibitors activity by molecular dynamics and free energy perturbation methods”, Mendeleev Commun., 30:4 (2020), 430–432
M. I. Lavrov, O. V. Stroganov, V. L. Zamoyski, V. V. Grigoriev, M. E. Zapolskiy, S. V. Sysolyatin, V. V. Malykhin, V. N. Surmachev, V. A. Palyulin, “Synthesis of an allosteric modulator of ionotropic glutamate receptors”, Mendeleev Commun., 30:2 (2020), 156–158
Polina N. Veremeeva, Irina V. Grishina, Olga V. Zaborova, Alexei D. Averin, Vladimir A. Palyulin, “Synthesis of 3,7-diacyl-1,5-dimethyl-3,7-diazabicyclo[3.3.1]nonane derivatives as promising lipid bilayer modifiers”, Tetrahedron, 75:33 (2019), 4444
M. I. Lavrov, P. N. Veremeeva, D. S. Karlov, V. L. Zamoyski, V. V. Grigoriev, V. A. Palyulin, “Tricyclic derivatives of bispidine as AMPA receptor allosteric modulators”, Mendeleev Commun., 29:6 (2019), 619–621