Synthesis and Evaluation of Anti-Epileptic Properties of New Phthalimide-4,5-Dihydrothiazole-Amide Derivatives

In this work, a novel series of phthalimide-4,5-dihydrothiazole-amide derivatives5a-fhave been synthesized and evaluated for their anti-epileptic activities against pentylenetetrazole (PTZ)-induced seizure in mice. Among the synthesized compounds, the most potent was 4-chloro derivative5bwith zero mortality in PTZ test. Molecular docking was performed to investigate the modes of interactions between GABA(A)receptor and synthetized compounds. Docking results were in good agreement with observed experimental data and indicate that among six new derivatives, compound5bwith highest effective anticonvulsant properties, had lowest binding energy. This compound also exhibited better anti-epileptic activity and lower binding energy for connect to GABA(A)receptor in comparison to thalidomide as standard anti-epileptic agent.

Automated summary

A novel series of phthalimide-4,5-dihydrothiazole-amide derivatives were synthesized and evaluated for their anti-epileptic activities. Compound 5b, a 4-chloro derivative, showed the most potent anti-epileptic activity with zero mortality in the experimental test. The molecular docking results confirmed its strong interaction with GABA(A) receptor, suggesting its potential as an effective anticonvulsant agent.