Органическая химия: текущие исследования
Открытый доступ

Абстрактный

Синтез и оценка противоэпилептической активности 5-бензоилоксиндола, нового фенитоинергического шаблона

Урбен К. Кассеэн, Фернан А. Гбагиди, Паскаль Карато, Кристофер Р. Маккарди и Жак Х. Пупар

Based on a rational approach using merely bioisosterism as euristic tool, we designed and tested a short series of congeners of 6-benzoyl-2(3H)-benzoxazolone as phenytoinergic lead. Among them, 5-benzoyloxindole showed an impressive activity in the Maximal Electroshock seizure test in mice at the same level of activity as phenytoin, carbamazepine and primidone, all these drugs nowadays considered worldwide as reference molecules, and only surpassed by ameltolide. Additional preliminary pharmacomodulations of this lead were unsuccessful. In view of its molecular concision and good druggability characteristics, 5-benzoyloxindole represents a valid platform for further medicinal chemistry elaborations.