Title:
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase. | Journal:
Bioorganic & medicinal chemistry letters. 2010 May;20(9):2828-31 | Authors:
Ronkin SM, Badia M, Bellon S, Grillot AL, Gross CH, Grossman TH, Mani N, Parsons JD, Stamos D, Trudeau M, Wei Y, Charifson PS. | Abstract:
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphylococcus aureus GyrB. | | See full PubMed entry: http://www.ncbi.nlm.nih.gov/pubmed/20356737 |
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BRAID