Departamento de Química Orgánica, Universidade de Vigo, 36310 Vigo, Spain.
Bioorg Med Chem Lett. 2010 Nov 15;20(22):6624-7. doi: 10.1016/j.bmcl.2010.09.031. Epub 2010 Sep 15.
New 6-substituted and 2,6-disubstituted pyridazinone derivatives were obtained starting from easily accessible alkyl furans by using oxidation with singlet oxygen to give 4-methoxy or 4-hydroxybutenolides, key intermediates of this synthetic strategy. The new pyridazinone derivatives have been studied as vasorelaxant and antiplatelet agents. Analysis of biological data revealed the silyl ethers (4a-i) and N,O-dibenzyl derivatives (6g-i) as the most active compounds.
新型 6-取代和 2,6-二取代哒嗪酮衍生物可由易得的烷基呋喃经单线态氧氧化得到 4-甲氧基或 4-羟基丁烯内酯，这是该合成策略的关键中间体。这些新型哒嗪酮衍生物被研究作为血管舒张剂和抗血小板剂。生物数据分析表明，硅醚（4a-i）和 N,O-二苄基衍生物（6g-i）是最具活性的化合物。
