ఆర్గానిక్ కెమిస్ట్రీ: ప్రస్తుత పరిశోధన
అందరికి ప్రవేశం

నైరూప్య

Synthesis and Antiepileptic Activity Assessment of 5-Benzoyloxindole, a Novel Phenytoinergic Template

ఉర్బైన్ సి. కస్సేహిన్, ఫెర్నాండ్ ఎ. గ్బగుయిడి, పాస్కల్ కరాటో, క్రిస్టోఫర్ ఆర్. మెక్‌కర్డీ మరియు జాక్వెస్ హెచ్. పౌపర్ట్

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.