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Design, synthesis, and in vitro, in vivo, and in silico evaluation of novel substituted 1,3,4-thiadiazole derivatives as anticonvulsant agents.


ABSTRACT: In the present study, a library of ten novel substituted 1,3,4-thiadiazole derivatives were designed and synthesized using an appropriate synthetic route. The characterization of the synthesized compounds was performed by FT-IR and NMR (1H and 13C) spectroscopy. The synthesized compounds were assayed for in vitro human carbonic anhydrase (CA) inhibition against two isoforms II and IX. The neurotoxicity of the synthesized derivatives was also evaluated using the rotarod test, along with their in vivo anticonvulsant activity, which was determined using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (sc-PTZ) methods. Although all the compounds showed good CA inhibition and anticonvulsant activity, two compounds 6d and 7

SUBMITTER: Anthwal T 

PROVIDER: S-EPMC11861159 | biostudies-literature | 2024

REPOSITORIES: biostudies-literature