Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376340 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
Ring-fused 2-pyridones, termed pilicides, are small synthetic 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 and tetrazoles significantly improve pilicide activity against uropathogenic E. coli.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Veronica Åberg, Pralay Das, Erik Chorell, Mattias Hedenström, Jerome S. Pinkner, Scott J. Hultgren, Fredrik Almqvist,