Hunt James C A, Briggs Emma, Clarke Eric D, Whittingham William G
Syngenta, Jealott's Hill International Research Centre, Bracknell, Berkshire RG42 6EY, UK.
Bioorg Med Chem Lett. 2007 Sep 15;17(18):5222-6. doi: 10.1016/j.bmcl.2007.06.076. Epub 2007 Jun 30.
A novel series of pyridothieno-1,2,3-triazines with potent antifungal activity against Erysiphe graminis f. sp. tritici has been discovered. Two complementary synthetic routes to compounds of this type have been developed and used to efficiently explore the structure-activity relationships around the lead compound. The incorporation of oxygen atoms into the side chains of the molecules has allowed the solubility of the compounds to be increased 10-fold whilst retaining biological activity.
已发现一系列新型吡啶并噻吩并-1,2,3-三嗪,它们对小麦白粉病菌具有强大的抗真菌活性。已开发出两种互补的合成路线来制备这类化合物,并用于有效地探索先导化合物周围的构效关系。将氧原子引入分子侧链可使化合物的溶解度提高10倍,同时保留生物活性。