Based on the strategy of diversity-oriented synthesis and the structures of natural product pimprinine and streptochlorin, two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties were efficiently synthesized under the optimized reaction conditions. Biological assays conducted at Syngenta showed the designed derivatives displayed an altered pattern of biological activity, of which 5h was identified as the most promising compound with strong activity against Pythium dissimile and also a broad antifungal spectrum in primary screening. Further structural optimization of pimprinine and streptochlorin derivatives is well under way, aiming to discover synthetic analogues with improved antifungal activity. Two series of novel pimprinine derivatives containing 1,3,4-oxadiazole-5-thioether moieties were efficiently synthesized through diversity-oriented synthesis strategy under the optimized conditions. Biological assays showed the designed derivatives exhibited potential activity.

中文翻译：

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具有 1,3,4-oxadiazole-5-thioether 部分的新型 pimprinine 衍生物的多样性导向合成和抗真菌活性。

基于多样性导向合成策略和天然产物pimprinine和链绿素的结构，在优化的反应条件下高效合成了含有1,3,4-恶二唑-5-硫醚部分的两个系列新型pimprinine衍生物。在先正达进行的生物测定表明，设计的衍生物显示出改变的生物活性模式，其中 5h 被确定为最有希望的化合物，对异化腐霉具有很强的活性，并且在初步筛选中具有广泛的抗真菌谱。pimprinine 和链绿素衍生物的进一步结构优化正在进行中，旨在发现具有改进抗真菌活性的合成类似物。两个系列的新型 pimprinine 衍生物含有 1,3, 在优化的条件下，通过面向多样性的合成策略有效地合成了 4-恶二唑-5-硫醚部分。生物测定表明设计的衍生物表现出潜在的活性。