A new series of N-[3-chloro-2-(substitutedphenyl)-4-oxo-azetidin-1-yl]isonicotinamide (2a-l) were synthesized through condensation reaction of isoniazide with substituted aldehyde. The newly synthesized compounds were characterized by spectral data (IR, (1)H NMR, mass spectra) and elemental analysis. Compound 2e exhibited excellent anticonvulsant activity and no neurotoxicity in comparison to reference drug phenytoin.