Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli
作者:Veronica Åberg、Pralay Das、Erik Chorell、Mattias Hedenström、Jerome S. Pinkner、Scott J. Hultgren、Fredrik Almqvist
DOI:10.1016/j.bmcl.2008.05.020
日期:2008.6
compounds that inhibit pilus assembly in uropathogenic Escherichia coli. Their biological activity is clearly dependent upon a carboxylic acid functionality. Here, we present the synthesis and biological evaluation of carboxylic acid isosteres, including, for example, tetrazoles, acyl sulfonamides, and hydroxamic acids of two lead 2-pyridones. Two independent biological evaluations show that acyl sulfonamides