Novel bivalent AMPA-receptor ligands of bis(pyrimidine) series

Nazarova, A.A.; Sedenkova, K.N.; Karlov, D.S.; Palyulin, V.А.; Averina, E.B.; Zamoyski, V.L.; Grigoriev, V.V.

Авторы: Nazarova A.A., Sedenkova K.N., Karlov D.S., Palyulin V.А., Averina E.B., Zamoyski V.L., Grigoriev V.V.
Сборник: 4th Russian Conference on Medicinal Chemistry MedChem Russia 2019, Ekaterinburg, Russia, June 10-14, 2019
Тезисы
Год издания: 2019
Место издания: Ekaterinburg, Russia
Первая страница: 82
Последняя страница: 82
Аннотация: AMPA-receptors are the attractive targets for treatment of a series of neurological disorders. Positive AMPA-receptors modulators can be useful for treatment of the cognitive impairments improving learning and memory, whereas in contrast negative modulators (or blockers) are perspective agents for treatment of epilepsy. Here we present the synthesis of a novel series of bispyrimidines 1 which were supposed to act as bivalent AMPA-receptors ligands. Based on our previously described synthetic approaches we obtained the targeted heterocycles 1 using two routes: (I) double SNAr reaction of 4-fluoropyrimidine N-oxides with different bisnucleophiles and subsequent reduction of N-oxide fragment, or (II) reduction of starting 4-fluoropyrimidine N-oxides and subsequent SNAr reaction with bisnucleophiles. Obtained compounds 1 were tested in patch-clamp experiments for the influence on the kainate-induced currents recorded for the Purkinje cells extracted from the rat cerebellum. Several compounds 1 showed high positive (increase of the kainate-induced currents for 35- 60% at 0.001‑0.1 μM) or negative modulating effect.
Добавил в систему: Радченко Евгений Валерьевич

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