Title:Importance of Pharmacophore in Designing Anticonvulsant Agents
Volume: 22
Issue: 4
Author(s): Amol Kale*, Rajendra Kakde, Smita Pawar, Vishal Jagtap and Rahul Dorugade
Affiliation:
- Department of Pharmaceutical Chemistry, Seth Govind Raghunath Sable College of Pharmacy, Saswad, Pune, Maharashtra
412301, India
- Sudhakarrao Naik Institute of Pharmacy, Pusad, Maharashtra 445204, India
Keywords:
Pharmacophore models, anticonvulsant, maximal electroshock seizure, drug development, electron donor, pharmacophoric features.
Abstract: Drug design is one of the critical aspects of the drug development process. The present
review focused on different heterocyclic molecules having anticonvulsant activity with structural
diversity and common pharmacophoric features. For the first time (1995), Dimmock and his team
introduced specific arrangements of three important pharmacophores for anticonvulsant activity. These
pharmacophores include two hydrophobic binding sites and one hydrogen binding site. After a few
years (2012), Pandeya modified Dimmock’s concept by adding one more pharmacophoric feature as
an electron donor in the previously suggested pharmacophoric arrangement of the anticonvulsant. As a
result, numerous scientists designed anticonvulsant drugs based on Dimmock’s and Pandeya’s concept.
In addition, marketed anticonvulsant preparation containing Riluzole, Phenobarbital, Progabide,
Ralitoline, etc., also holds the suggested pharmacophores by Dimmock and Pandeya’s pharmacophoric
concept. This review mainly focuses on the compilation of reported scientific literature in the last decade
on the pharmacophoric features of different heterocyclic anticonvulsants, which will help develop
new anticonvulsants.