Marcin Jakubiec, Michał Abram, Mirosław Zagaja, Marta Andres-Mach, Joanna Szala-Rycaj, Gniewomir Latacz, Ewelina Honkisz-Orzechowska, Szczepan Mogilski, Monika Kubacka, Małgorzata Szafarz, Krzysztof Pociecha, Katarzyna Przejczowska-Pomierny, Elżbieta Wyska, Katarzyna Socała, Dorota Nieoczym, Bartłomiej Szulczyk, Piotr Wlaź, Cameron S Metcalf, Karen Wilcox, Rafał M Kamiński, Krzysztof Kamiński
In the present study, a series of original alaninamide derivatives have been designed applying a combinatorial chemistry approach, synthesized, and characterized in the in vivo and in vitro assays. The obtained molecules showed potent and broad-spectrum activity in basic seizure models, namely, the maximal electroshock (MES) test, the 6 Hz (32 mA) seizure model, and notably, the 6 Hz (44 mA) model of pharmacoresistant seizures. Most potent compounds 26 and 28 displayed the following pharmacological values: ED50 = 64...
May 14, 2024: ACS Chemical Neuroscience