Organic Chemistry: Current Research
Open Access
ISSN: 2161-0401
+44 1478 350008
ISSN: 2161-0401
+44 1478 350008
Urbain C. Kasséhin
Medicinal Chemistry, Louvain Drug Research Institute, Unité de Chimie Pharmaceutique et Radiopharmacie,
Belgium
Research Article
Synthesis and Antiepileptic Activity Assessment of 5-Benzoyloxindole, a Novel Phenytoinergic Template
Author(s): Urbain C. Kasséhin, Fernand A. Gbaguidi, Pascal Carato, Christopher R. McCurdy and Jacques H. PoupaertUrbain C. Kasséhin, Fernand A. Gbaguidi, Pascal Carato, Christopher R. McCurdy and Jacques H. Poupaert
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... View More»
DOI:
10.4172/2161-0401.1000133