Updates on the Synthetic Strategies and Structure-Activity Relationship of Anticonvulsant Benzothiazole and Benzimidazole Derivatives

Epilepsy is a chronic neurological disorder characterized by periodic and unpredictable seizures affecting the neurobiological, psychological, cognitive, economic, and social well-being of patients. It is one of the causes of concern in developed as well as developing countries as currently marketed drugs are not capable of providing protection against it. Although several heterocyclic moieties have been frequently used as building blocks for the preparation of anticonvulsant drugs, more focused and consistent research on the synthesis of potential molecules with less adverse effects is the need of the hour. It can be concluded on the basis of available research reports that among several heterocyclic compounds, benzo-fused five-membered heterocyclic moieties (benzothiazole and benzimidazole) have been utilized far less than their great potential as building blocks for the synthesis of anticonvulsant drugs. Various reports clearly established that the required pharmacophore model could be easily achieved through benzothiazole and benzimidazole moieties as two hetero atoms and aryl rings are present in the structure. The present study highlights various synthetic approaches for anticonvulsant benzothiazole and benzimidazole derivatives with their structure-activity relationship studies in order to provide a trove of knowledge to medicinal chemists for future research.