Anticonvulsant activity of novel 1-(morpholinomethyl)-3-substituted isatin derivatives

• A variety of novel isatin derivatives were synthesized and characterized.
• Investigated for antiepileptic activity using MES and scPTZ seizures tests.
• Compound 6f emerged out as the pilot molecule.

A variety of novel isatin derivatives 5a–5j and 6a–6j were synthesized and characterized by spectroscopic means and elemental analysis. The title compounds were investigated for antiepileptic activity using MES and scPTZ seizures tests. Neurotoxicity study was performed by the rotorod test. The relationship between the functional group variation and the biological activity of the evaluated compounds was discussed. Among the synthesized analogs, the most active one was 6f that revealed protection in MES at a dose of 30 mg/kg (i.p.) after 0.5 h and 4 h. This molecule also provided protection in the scPTZ at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h).

Figure optionsDownload as PowerPoint slide