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

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).

The regioselective synthesis of 1-heteroaryl-3H/methyl-5-amino-4-phenylpyrazoles 3a–n was achieved by the treatment of heteroarylhydrazines 1a–g with α-phenylacylacetonitrile 2a–b, respectively. The structures of the compounds 3 were established by the combined use of 1H and 13C NMR spectroscopy. All the 14 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).Figure optionsDownload as PowerPoint slide