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Ethyl Imidazole-1-Carboxylate as a Novel Carbonylating Agent for the Synthesis of 1,2,4-Oxadiazol-5(4H)-Ones and Evaluation of their Anti-Mycobacterial Activity

Indrasena Reddy K*, Aruna C, Sudhakar Babu K, Yogeeswari P, and Sriram D

Various highly substituted 1,2,4-oxadiazol-5(4H)-ones were synthesized from the corresponding amidoximes using ethyl imidazole-1-carboxylate (EImC) as a novel carbonylation agent. This method is simple and convenient to produce these biologically interesting heterocycles in high yields. Among them, 4a, 4b, 4c, 4e, 4f, 4h, and 4i are identified as lead molecules. In particular, 4e, and 4h are found to display promising activity as good as ciprofloxacin, whereas 4i showed an excellent activity, which is equal to the IC50 value of ethambutol against Mycobacterium tuberculosis.