Synthesis of 2-[4-(substituted benzylidene)-5-Oxo- 4,5-dihydro-oxazol-2-ylmethyl]-isoindole-1,3-dione Derivatives as Novel Potential Antimicrobial Agents

In the present study, a series of new substituted oxazolone derivatives (4a-4h) were synthesized by the Erlenmeyer condensation of phthaloylglycylglycine with different aldehydes in the presence of anhydrous sodium acetate and acetic anhydride. The structure of newly-synthesized compounds were evaluated by elemental analyses and spectral (UV-Visible, IR, NMR, Mass) studies. All the synthesized derivatives were evaluated for their antimicrobial activity. Preliminary pharmacological evaluation revealed that the compound 4b, 4c, 4d, 4g and 4h showed better performance against Staphylococcus aureus, Staphylococcus epidermidis, Proteus mirabilis, Pseudomonas aeruginosa, Candida albicans and Aspergillus niger. The minimum inhibitory concentration (MIC) was determined for the target compounds as well as for standard drugs. Physicochemical similarity of the new derivatives with standard drugs was assessed by calculating from a set of 10 physicochemical parameters using software programs.The result demonstrated the potential and usefulness of developing novel oxazolone derivatives which would be effective against resistant and pathogenic bacterial and fungal strain. Keywords: Oxazolone; Substituted benzylidene; Antibacterial activity; Antifungal activity