Jiangsu Key Laboratory of Pesticide Science, College of Sciences, Nanjing Agricultural University, Nanjing, 210095, China.
Syngenta Jealott's Hill International Research Centre, Bracknell, Berkshire, RG42 6EY, UK.
Mol Divers. 2021 Feb;25(1):205-221. doi: 10.1007/s11030-020-10048-8. Epub 2020 Feb 13.
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.
基于多样性导向合成策略以及天然产物 pimprinine 和 streptochlorin 的结构，我们在优化的反应条件下高效合成了两个含有 1,3,4-噁二唑-5-硫醚部分的新型 pimprinine 衍生物系列。在先正达公司进行的生物测定表明，所设计的衍生物显示出改变的生物活性模式，其中 5h 被鉴定为最有前途的化合物，对 Pythium dissimile 具有很强的活性，并且在初步筛选中具有广泛的抗真菌谱。目前正在对 pimprinine 和 streptochlorin 衍生物进行进一步的结构优化，旨在发现具有改善的抗真菌活性的合成类似物。通过优化条件下的多样性导向合成策略，我们高效合成了两个含有 1,3,4-噁二唑-5-硫醚部分的新型 pimprinine 衍生物系列。生物测定表明，所设计的衍生物表现出潜在的活性。
