• 1 Department of Child Healthcare, Shandong Provincial Third Hospital, Cheeloo College of Medicine, Shandong University, Jinan, China
  • 2 Innoscience Research Sdn Bhd, Subang Jaya, Malaysia
Neuroimmunomodulation, 2021;28(2):90-98.
PMID: 33774633 DOI: 10.1159/000513297


INTRODUCTION: Pediatric patients with epilepsy are prone to cognitive impairments during growth and long-term use of most antiepileptic drugs (AED). The affected children do not respond to conventional AED and may require novel drugs to manage the disease. Valproic acid, a first-line drug to treat epilepsy, is associated with serious side effects, which precludes its wider use. Thus, in the present study, we intended to develop novel substituted pyrazoles.

METHODS: The molecules were tested for anticonvulsive activity in Swiss albino mice via maximal electroshock seizure and subcutaneous pentylenetetrazole assays. The most potent molecule among the class was further assayed for its effect on behavioral and CNS depressant activity. The effect of the most potent compounds was also analyzed on various indices of oxidative stress and inflammation in mice.

RESULTS: The designed compounds showed significant anticonvulsive activity in mice revealing 7h as the most potent anticonvulsive agent. The most potent anticonvulsant molecule 7h further showed no behavioral alteration and considerable CNS depressant activity. It also reduces the level of oxidative stress and inflammation in the mice.

CONCLUSION: Our study demonstrated utility of pyrazole derivatives as anticonvulsants against epilepsy.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.