alexa Synthesis and Antiepileptic Activity Assessment of 5-Benzoyloxindole, a Novel Phenytoinergic Template | OMICS International| Abstract

ISSN: 2161-0401

Organic Chemistry: Current Research

  • Research Article   
  • Organic Chem Curr Res 2014, Vol 4(1): 133
  • DOI: 10.4172/2161-0401.1000133

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

Urbain C. Kasséhin1,2*, Fernand A. Gbaguidi2, Pascal Carato3, Christopher R. McCurdy4 and Jacques H. Poupaert1
1Medicinal Chemistry, Louvain Drug Research Institute, Unité de Chimie Pharmaceutique et Radiopharmacie, Université catholique de Louvain, 73, Bte B1.73.10, Av. E. Mounier B-1200 Bruxelles, Belgium
2Laboratoire de Chimie Pharmaceutique Organique, Ecole de Pharmacie, Faculté des Sciences de la Santé, University of Abomey-Calavi, Campus du Champ de Foire ,01 BP 188, Benin
3Medicinal Chemistry, Laboratoire de Chimie Thérapeutique (EA 4481) 3, Faculté de Pharmacie, Département de Pharmacologie Médicale, Université Lille Nord de France, Rue du Professeur Laguesse, BP83, 59006 Lille, France
4Medicinal Chemistry, School of Pharmacy, University of Mississipi, 419 Faser Hall, PO BOX 1848, 386771848, USA
*Corresponding Author : Urbain C. Kasséhin, Medicinal Chemistry, Louvain Drug Research Institute, Unité de Chimie Pharmaceutique et Radiopharmacie, Université catholique de Louvain, Belgium, Tel: +32 (0) 489 684972 or +229 95 84 52 07, Email: [email protected]

Received Date: Oct 21, 2014 / Accepted Date: Jan 04, 2015 / Published Date: Jan 08, 2015

Abstract

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.

Keywords: Antiepileptic activity; 5-benzoyloxindole; Phenytoinergic drugs; Bioisosteric substitution

Citation: Kasséhin UC, Gbaguidi FA, Carato P, McCurdy CR, Poupaert JH (2015) Synthesis and Antiepileptic Activity Assessment of 5-Benzoyloxindole, a Novel Phenytoinergic Template. Organic Chem Curr Res 4: 133. Doi: 10.4172/2161-0401.1000133

Copyright: © 2015 Kasséhin UC, et al. This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

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