Biologically active compounds with heteroaromatic ring system of Cefuroxime axetil have been synthesized via aminomethylation reaction. The aminomethylation of Cefuroxime axetil with various biologically potent sulphonamides / secondary amines was carried out and then characterized by elemental analysis and spectral studies – IR, 1H-NMR and 13C-NMR. The compounds were screened for their antibacterial activity against various pathogenic bacteria at varying concentrations. The antibacterial activity of Cefuroxime axetil derivatives was compare with parent sulphonamides. The toxicity of synthesized Cefuroxime axetil derivatives was ascertained by LD50 test.