We report herein the synthesis and biological activity of a new kind of azetidinone derivatives of benzotriazole. The reaction was carried out by both conventional and microwave methods. The chemical structures of all the synthesized compounds were deduced according to FTIR, 1 H NMR, 13 C NMR and FAB-mass spectral along with microanalytical data. All the synthesized compounds of series 5a–i were evaluated for their antitubercular activity against Mycobacterium tuberculosis H37RV and antimicrobial activity against some selected microorganism. Unexpectedly, some azetidinone derivatives of benzotriazole displayed better activities.