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The synthesis of biologically active molecules carried out by using Aminothiazole nuclei and their various derivatives as precursors. In present work, Schiff’s bases (27-36) were prepared by reacting amino group of thiazole moiety (26) with various aromatic aldehydes. The titled, novel 2-substituted aminothiazoles (37-46) were obtained by reaction of these Schiff’s bases with benzil by providing excess amount of ammonium acetate (NH4OAc). Structure elucidation of all the newly synthesized compounds was carried out by employing elemental analysis, FT-IR, 1H NMR and Mass spectrometry. The newly synthesized novel 2-substituted-aminothiazoles were screened for their anti-bacterial activity against two gram +ve bacterial strains viz. Staphylococcus aureus and Bacillus subtilis and against a gram –ve bacterial strain viz. Escherichia coli and for anti-fungal activity against two fungal strains viz. Candida albicans and Aspergillus niger using cup plate method by using Norfloxacin and Fluconazole as standard drugs respectively. Cyto-toxic activity of the synthesized compounds was evaluated by determining the percentage growth inhibition of Daltonꞌs Lymphoma Ascites (DLA) cells and Erlichꞌs Ascites Carcinoma (EAC) cells by Tryphan Blue Dye Exclusion technique. Results of biological activity studies indicated that the newly synthesized 2-substituted aminothiazoles displayed good anti-bacterial activity against gram –ve bacterial strain Escherichia coli and anti-fungal activity against Candida albicans. Further, these compounds were found to show significant percent growth inhibition against DLA and EAC, cell-lines.