Synthesis and SAR studies of novel antifungal 1,2,3-triazines
Synthesis and SAR studies of novel antifungal 1,2,3-triazines
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DOI：
10.1016/j.bmcl.2007.06.076
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发表时间：
2007-09-15
影响因子：
2.7
通讯作者：
Whittingham, William G.
中科院分区：
文献类型：
--
作者：
Hunt, James C. A.;Briggs, Emma;Whittingham, William G.
发现了一系列新的对小麦白粉病菌（Erysiphe graminis f sp. triacetylene）具有有效抗真菌活性的吡啶并噻吩并-1，2，3-三嗪类化合物。已经开发了这种类型的化合物的两种互补的合成路线，并用于有效地探索先导化合物周围的结构-活性关系。将氧原子掺入分子的侧链中使得化合物的溶解度增加10倍，同时保持生物活性。(c)2007爱思唯尔有限公司保留所有权利。
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. (c) 2007 Elsevier Ltd. All rights reserved.