Synthesis and Evaluation of Novel [1,2,4]Triazolo[1,5-c]quinazoline Derivatives as Antibacterial Agents

2017 
A series of new 2-aryl-5-methyl-[1,2,4]triazolo[1,5-c]quinazoline derivatives (5a–5g) have been synthesized by the reaction of 3-amino-2-methylquinazolin-4-(3H)-one (3) with aromatic nitriles in potassium tert-butoxide under reflux conditions. 3-Amino-2-methylquinazolin-4-(3H)-one (3) was synthesized by the reaction 2-methyl-4H-benzo[d][1,3]oxazin-4-one (2) with hydrazine hydrate. The chemical structure of products was confirmed by IR, 1H, 13C NMR and elemental analysis. These compounds were screened for antibacterial [Staphylococcus aureus (ATCC 25923), Bacillus cereus (ATCC 11778), Micrococcus luteus (ATCC 9341), Escherichia coli (ATCC 25922), and Pseudomonas aeruginosa (ATCC 27853)] activities, using the zone inhibition method.
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