In the present study we have reviewed the synthesis and different biological activities of some azetidinone derivatives. A series of new azetidinone class of bioactive agents based on imidazol-4-one nucleus have been synthesized by a simple and efficient synthetic protocol. The 3-(4-amino-phenyl)-5-benzylidene-2-methyl-3,5- dihydro-imidazol-4-one nucleus formed from 4-benzylidene-2-methyl-4H-oxazol-5one using p-phynelenediamine in pyridine followed by reaction with various substituted aromatic aldehyde to form the corresponding Schiff base intermediates. Effort has been made to derive final azetidinone analogues from Schiff bases by using chloroacetyl chloride. Newer analogues were characterized by IR, 1H NMR, and elemental analyses. The newly synthesized analogues were then examined for their antimicrobial activity against some bacterial and fungal strains to develop a novel class of antimicrobial agents.