Počet záznamů: 1
Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents
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SYSNO ASEP 0422133 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents Tvůrce(i) Sahoo, B. M. (IN)
Dinda, S. C. (IN)
Kumar, B. V. V. R. (IN)
Panda, J. R. (IN)
Brahmkshatriya, Pathik (UOCHB-X)Celkový počet autorů 5 Zdroj.dok. Mini - Reviews in Medicinal Chemistry - ISSN 1389-5575
Roč. 13, č. 14 (2013), s. 2076-2081Poč.str. 6 s. Jazyk dok. eng - angličtina Země vyd. NL - Nizozemsko Klíč. slova antiepileptic activity ; docking study ; epilepsy ; green synthesis ; neurotoxicity ; thiadiazole Vědní obor RIV CC - Organická chemie Institucionální podpora UOCHB-X - RVO:61388963 UT WOS 000328088300008 EID SCOPUS 84892955771 DOI 10.2174/13895575113136660099 Anotace 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. Pracoviště Ústav organické chemie a biochemie Kontakt asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Jana Procházková, Tel.: 220 183 418 Rok sběru 2014
Počet záznamů: 1