Department of Chemistry, Umeå University, SE-90187 Umeå, Sweden.
J Org Chem. 2011 Dec 2;76(23):9817-25. doi: 10.1021/jo201952p. Epub 2011 Oct 31.
Ringfused bicyclic 2-pyridones exhibit interesting biological properties against pili assembly in uropathogenic Escherichia coli (Pinkner, J. S. et al. Proc. Natl. Acad. Sci. U. S. A.2006, 103, 17897-17902; Åberg, V. et al. Org. Biomol. Chem.2007, 5, 1827-1834) as well as curli formation (Cegelski, L. et al. Nat. Chem. Biol.2009, 5, 913-919). In the search for new ring-fused central fragments, highly selective synthetic routes to the 2-furanone or 2-pyrone containing tricyclic scaffolds 1 and 2 have been developed.
具有环稠合双环 2-吡啶酮结构的化合物对尿路致病性大肠杆菌的菌毛组装（Pinkner, J. S. 等人，Proc. Natl. Acad. Sci. U. S. A.2006, 103, 17897-17902; Åberg, V. 等人，Org. Biomol. Chem.2007, 5, 1827-1834）以及卷曲菌毛形成（Cegelski, L. 等人，Nat. Chem. Biol.2009, 5, 913-919）具有有趣的生物活性。为了寻找新的环稠合中心片段，我们开发了高度选择性的合成路线，用于构建含有 2-呋喃酮或 2-吡喃酮的三环支架 1 和 2。
