An Important Potential Anti-Epileptic/Anticonvulsant Active Group: A Review of 1,2,4-Triazole Groups and Their Action

Epilepsy is one of the most common encountered neurological disorders. Many individuals continue to have seizures despite medical and surgical treatments, suggesting new antiepileptic/anticonvulsant drugs are required. Triazole compounds are widely used in pharmaceuticals and have gained significant importance in medicinal chemistry. This article is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades through extensive literature research. The results show that triazole occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their capability to exhibit an array of properties and bioactivities, Therefore, 1,2,4-triazole seems to be an important pharmacophore, especially in the field of antiepileptic, which is of great explored potentiality and utilized value. Through in-depth research on this type of structure, it is believed that more 1,2,4-triazole compounds will be developed as anti-epileptic drugs for clinical use.

Ethnobotanical Research of Plants Used in Traditional Medicine for The Treatment of Epilepsy in Southern Mozambique

Background Epilepsy is a chronic brain disease that affects about 50 million people worldwide, mainly in developing countries. It is treated with anticonvulsant drugs, but in some cases, conventional anticonvulsants have not been effective, leading patients to turn to alternative herbal treatments. The study aimed to identify plants used in traditional medicine for the treatment of epilepsy in southern Mozambique, record the parts used, the method of preparation as well as the mode of administration. Methodology: The study was conducted between April to June 2019. 53 Traditional Medicine Practitioners were interviewed using a semi-structured questionnaire. The data was analyzed by calculating the Percentage of Citation (%FC) and Informant Factor Consensus (IFC). Results A total of 32 medicinal plants belonging to 18 botanical families were identified for the treatment of epilepsy in the southern part of Mozambique. The species, Hugonia orientalis Engl (22.64%), Maclura africana Bur (16.98%), Strychnos spinosa Lam (13.21%), Terminalia sericea Bruch ex DC (13.21%) and Manilkara mochisia (Bark) Dubard (11.32%) were the most cited. The families Annonaceae and Menispermaceae (4 species) were the most representative in number of species. The root was the most commonly used plant part (54.2%), the frequently used preparation mode was decoction (71%), and administration of the remedies was often by oral route. Conclusion Medicinal plants still play an important role in primary health care in the study area. However there is a need to develop pharmacological studies based on these plants to understand the mechanism of action of the bioactive compounds and for the future development of new and more effective anticonvulsant drugs

Computational and Synthetic Target-Based Approaches to the Discovery of Novel Anticonvulsant Compounds

Background: During the past decades, an important number of anticonvulsant drugs have been incorporated into the collection of drugs to treat epilepsy. However, two main difficulties remain unsolved in therapy: the development of drug-resistant epilepsy and the occurrence of severe toxic effects caused by the medication in responsive patients. The retrospective analysis of the strategies for discovering known anticonvulsant drugs showed that screening campaigns on animal models of epilepsy had been almost the exclusive strategy for identifying the marketed compounds. However, the actual structural and functional information about the molecular targets of the anticonvulsant drugs, and the increasing knowledge of the molecular alterations that generate epileptic seizures, allow a more rational identification of active compounds. Objective: This review compiles target-based strategies used for the discovery of new anticonvulsant candidates and is divided into two main topics. The first one provides an overview of the computational approaches (docking-based virtual screening and molecular dynamics) to find anticonvulsant structures that interact with the voltage-gated ion channels and the enzyme carbonic anhydrase. The second one includes the analysis of active compounds synthesized to act simultaneously on different molecular targets by a combination of pharmacophores of anticonvulsant drugs. Conclusion: Current knowledge of the architectures of anticonvulsant targets makes computational simulations attractive methods for the discovery and optimization of active compounds. Combining the results achieved by virtual screening on different targets could lead to multitarget compounds as an alternative to the design of structures that merge scaffolds of known drugs.