Synthesis and antibacterial activity of some new 1-heteroaryl-5-amino-3H/methyl-4-phenylpyrazoles Original Research Article

The regioselective synthesis of 1-heteroaryl-5-amino-4-phenylpyrazoles 3a–g and 1-heteroaryl-5-amino-3-methyl-4-phenylpyrazoles 3h–n was achieved by the treatment of heteroarylhydrazines 1a–g with α-phenylformylacetonitrile 2a and α-phenylacetylacetonitrile 2b, respectively. The structures of the compounds 3 were established by the combined use of 1H and 13C NMR spectroscopy. All the fourteen compounds were tested for their in vitro antibacterial activity against three Gram-positive and two Gram-negative bacteria. Six compounds 3a, 3d, 3e, 3g, 3l, and 3n from this series were found to be equipotent or more potent than the commercial antibiotics (Linezolid and Cefroxime axetil).