Carboxylic acid isosteres improve the activity of ring-fused 2-pyridones that inhibit pilus biogenesis in E. coli
2008 (English)In: Bioorganic & Medicinal Chemistry Letters, Vol. 18, no 12, 3536-3540 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
Elsevier Ltd , 2008. Vol. 18, no 12, 3536-3540 p.
2-Pyridone, Bioisostere, Antimicrobial, Pili, Escherichia coli, Pilicide
IdentifiersURN: urn:nbn:se:umu:diva-9676DOI: 10.1016/j.bmcl.2008.05.020OAI: oai:DiVA.org:umu-9676DiVA: diva2:149347