Synthesis, spectroscopic characterization and pharmacological evaluation of oxazolone derivatives
2013
A series of six 4-(arylmethylidene)-2-phenyl/methyl-5(4H)-oxazo- lone derivatives were synthesized using a reported method by condensation of aldehydes with N-benzoyl/N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. Five of the compounds are new derivatives. The structures of the compounds were eva- luated based on 1 H-NMR, 13 C-NMR, EI-MS and FT-IR spectroscopy and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. The antibacterial activity was tested by the agar well diffusion method using Mueller-Hinton agar medium. Compound 2 showed excellent activity against Staphylococcus aureus exhibiting 16 mm (80 %) inhi- bition and above 24 mm (70 %) against Salmonella typhi. Compound 6 was the most active compound against Escherichia coli having 20 mm (80 %) inhi- bition followed by compound 5 having above 18 mm (70 %) inhibition. Urease inhibition activity of all the compounds was determined by the indophenol method. Compounds 3, 6 and 7 showed significant inhibition against Jack bean urease.
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