Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents

0422133 - ÚOCHB 2014 RIV NL eng J - Článek v odborném periodiku
Sahoo, B. M. - Dinda, S. C. - Kumar, B. V. V. R. - Panda, J. R. - Brahmkshatriya, Pathik
Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents.
Mini - Reviews in Medicinal Chemistry. Roč. 13, č. 14 (2013), s. 2076-2081. ISSN 1389-5575. E-ISSN 1875-5607
Institucionální podpora: RVO:61388963
Klíčová slova: antiepileptic activity * docking study * epilepsy * green synthesis * neurotoxicity * thiadiazole
Kód oboru RIV: CC - Organická chemie
Impakt faktor: 3.186, rok: 2013

Epilepsy is one of the commonly occurring chronic neurological disorders which involves abnormal electrical impulses in the brain. It is characterized by the sudden loss of consciousness, followed by abnormal shaking of the body. Though there are various types of antiepileptic drugs available clinically, the treatment of epilepsy still remains inadequate because of their toxicity and idiosyncratic side effects. Thus, there is unmet medical need to develop safe drugs for the treatment of epilepsy with lower side effects and improved bioavailability profiles. Considering the structural similarity between phenytoin/lamotrigine, a series of 1,3,4-thiadiazole was designed based on molecular docking study into the active site of the voltage-gated sodium channels. Antiepileptic activity of the synthesized compounds was evaluated in rats by maximal electroshock induced seizures (MES) model at different doses. Among the tested compounds, some exhibited significant anticonvulsant activity as compared to phenytoin in a dose-dependent manner. The neurotoxicity study was carried out using the rotarod test and the results of which suggests that the target compounds are safe and could be further developed as potential lead for antiepileptic drugs.
Trvalý link: http://hdl.handle.net/11104/0228358