Turk J Pharm Sci 12(1), 39-44, 2015 39 Original article Synthesis and Antibacterial Activity of Some Azetidinone Derivatives Containing 2-Amino 6,7 Substituted Benzothiazole Sibaji SARKAR* 1 , Rajani CHAUHAN 2 , Jaya DWIVEDI 3 1 N. R Vekaria Institute of Pharmacy, C.L College Campus, Junagadh, Gujarat- 362001, INDIA 2 Banasthali University, Department of Pharmacy , Rajasthan - 304022, INDIA 3 Banasthali University, Department of Chemistry, Rajasthan -304022, INDIA A novel series of azetidinone AZ1-6 been prepared from the building blocks 2, 3, 4 (trisubstituted benzaldehyde)-N-(6,7 substituted-1,3-benzothiazol-2-yl) semicarbazone [2.026a-o]. All of the synthesized compounds have been confirmed by elemental analyses, IR and 1 H NMR spectral data. These newly synthesized compounds were screened for their antibacterial activity. Variable and modest activity was observed against the investigated strains of bacteria, however compounds AZ2, AZ3, AZ5 and AZ6 revealed significant antibacterial activity against Bacillus subtilis and Pseudomonas compared to the reference drug Procaine penicillin and Streptomycin. Key words: Schiff base, Azetidinone, 2-Amino 6,7 substituted benzothiazole , Antibacterial activity. 2-Amino-6,7-Sübstitüe Benzotiyazol İçeren Bazı Azetidinon Türevlerinin Sentezi ve Antibakteriyel Aktiviteleri 2, 3, 4 (trisübstitüe benzaldehit)-N-(6, 7 sübstitüe-1,3-benzotiyazol-2-il) semikarbazon [2.026a-o] dan hareketle yeni bir seri azetidinon (AZ1-6) türevi hazırlanmıştır. Sentezlenen bileşiklerin yapıları elemental analiz, IR ve 1 H NMR verileriyle kanıtlanmış ve antibakteriyel aktiviteleri denenmiştir. Bileşiklerden AZ2, AZ3, AZ5 ve AZ6 Bacillus subtilis ve Pseudomona’a karşı referans bileşikler Prokain penisilin ve Streptomisin ile kıyaslandıklarında kayda değer aktiviteye sahip bulunmuştur. *Correspondence: E-mail: sibajisarkar004@gmail.com INTRODUCTION The number of life threatening infections caused by multidrug resistant Gram-positive and Gram-negative pathogens has reached an alarming level in hospitals and the community. Infections caused by these organisms create a serious challenge to the scientific community and the need for an effective therapy has led to a search for novel antibacterial agents. Various famous antibiotics like penicillins, cephalosporins and carbapenems are associated with antitumor (1) anti- inflammatory (2) antituberculer (3) activity due to the presence of 2-azetidinone ring in them. Similarly benzothiazole also have considerable attention because of their various biological and pharmacological activities like antituberculer (4), antimicrobial (5), anti- inflammatory (6). Small ring heterocycles containing nitrogen, sulfur and oxygen gained great importance since a long time due to their important medicinal properties. It is well known that when one biologically active molecule linked to other, the resultant molecule generally has increase the potency. Therefore it was thought worthwhile to synthesize better kinds of drugs by incorporating azetidinone in benzothiazole moiety. Keeping in view of diverse activity of benzothiazole and azetidinone nucleus, it is planned to synthesis the title compound and screens them for their possible antibacterial activities.