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2-Azetidinone shows biological activities like anti-bacterial, anti-microbial activity, anti-tubercular activity, and anti-cancer activity. 2-azetdinone derivatives were synthesized by simple procedures. The first step is synthesis of benzohydrazide through nucleophilic substitution reaction between methyl benzoate and hydrazine hydrate. The above formed compound is then treated with substituted aromatic aldehydes in the presence of catalytic amount of concentrated hydrochloric acid with stirring for one hour to give benzohydrazone which results in the formation of Schiff bases.Schiff bases undergone cyclisation in the presence of chloroacetylchloride and diethylenediamine by using ethanol as a solvent upon stirring for 4 hour’s yielded 2-azetidinone derivatives. The in-silico anti-leukemic activity was determined by using the computational tools i.e. “PASS Online”, “AutoDock4.2” and “ADMET” properties by online software’s. Among these six derivatives compounds (AZT-6) was shown more activity when compared with the other five compounds.