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

摘要

> 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‐(3 H )‐one ( 3 ) with aromatic nitriles in potassium tert ‐butoxide under reflux conditions. 3‐Amino‐2‐methylquinazolin‐4‐(3 H )‐one ( 3 ) was synthesized by the reaction 2‐methyl‐4 H ‐benzo[ d ][1,3]oxazin‐4‐one ( 2 ) with hydrazine hydrate. The chemical structure of products was confirmed by IR, 1 H, 13 C 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.