作者:Singh, Himanshu、Kumar, Rajnish、Mazumder, Avijit、Salahuddin、Kumar Yadav, Ranjeet、Kukreti, Neelima、Abdullah, Mohd. Mustaqeem、Kumar Tyagi, Pankaj、Chaitanya
DOI:10.1002/cbdv.202400642
日期:——
New 2‐(4‐benzothiazol‐2‐yl‐phenoxy)‐1‐(3,5‐diphenyl‐4,5‐dihydro‐pyrazol‐1‐yl)‐ethanones (9a‐o) have been designed and synthesized. The antiepileptic potential of the synthesized compounds has been tested by following standard animal screening models which include maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models. The study concluded that compounds 9c, 9d, 9f, 9i, 9n, and 9o possessed good antiepileptic potential when compared with standard drugs like carbamazepine and phenytoin. The results of the rotarod performance test also established them without any neurotoxicity. The motor impairment test yielded that the synthesized compounds are also good antidepressants. In‐silico studies have been performed to determine the eligibility of synthesized compounds as orally administered molecules and interactions with the target proteins. The result of in‐silico studies reinforced results obtained by in vivo study of the synthesized compounds along with their possible mechanism of antiepileptic action i.e. via inhibiting voltage‐gated sodium channels (VGSCs) and gamma‐aminobutyric acid‐A receptor.