Synthetic Organic Chemistry Laboratory, Department of Chemistry, Dr. H. S. Gour University, Sagar-470 003, Madhya Pradesh, India E-mail : professorsks@rediffmail.com Manuscript received 17 March 2006, revised 25 July 2006, accepted 7 September 2006 Indole on reaction with chloroacetyl chloride afforded N1-(1-chloro acetyl)-indole which was renuxed with hydrazine hydrate to give N1-[(1-hydrazino)acetyl]-indole. The hydrazino derivative of indole was further treated with various substituted aromatic carbonyls to get N1-[(benzylidene hydrazino)-acetyl]-indoles (3a-j). The compounds 3a-j were treated with chloroacetyl chloride in presence of Et3N to afford N1-[(2-oxo-3-chloro-4-aryl-azitidin)-(acetyl amino)] -indoles,4a-j. The structures of all the compounds were elucidated by elemental analysis, IR and 1H NMR spectrometry. All the compounds were screened for their antimicrobial, anti-iunammatory and anticonvulsant activities.