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.