新型含嘧啶环的半乳糖苷类衍生物的合成及杀菌活性

陈美航; 鲁道旺; 张迅; 杜士杰; 李娜; 马关康; 吴文能; 罗海荣

doi:10.16801/j.issn.1008-7303.2021.0112

新型含嘧啶环的半乳糖苷类衍生物的合成及杀菌活性

Synthesis and antimicrobial activities of novel galactoside derivatives containing a pyrimidine moiety

摘要

摘要: 为寻找具有更高杀菌活性的含氮杂环化合物，合成了13个未见文献报道的新型含嘧啶环的半乳糖苷类衍生物，其结构经过核磁共振氢谱 (¹H NMR)、碳谱 (¹³C NMR) 和高分辨质谱 (HRMS) 等方法确证。杀菌活性测试结果表明：该类化合物对马铃薯晚疫病菌Phytophthora infestans、小麦赤霉病菌Gibberella zeae、水稻纹枯病菌Thanatephorus cucumeris、葡萄座腔病菌Botryosphaeria dothidea和拟茎点霉菌Phompsis sp. 均具有较好的杀菌活性，其中化合物 4m 对马铃薯晚疫病菌的EC₅₀值分别为8.67 μg/mL，与对照药剂烯酰吗啉 (EC₅₀值8.34 μg/mL) 活性相当。此外，该类化合物对柑橘溃疡病菌Xanthomonas citri subsp. citri和水稻白叶枯病菌Xanthomonas oryzae pv. oryzae也有一定的杀菌活性。

Abstract: To find nitrogen heterocyclic derivatives with higher antimicrobial activities, thirteen novel galactoside derivatives containing a pyrimidine moiety were synthesized, and their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The result of biological activity indicated that the target compounds possessed good antifungal activities against Phytophthora infestans, Gibberella zeae, Thanatephorus cucumeris, Botryosphaeria dothidea and Phompsis sp.. Among them, compound 4m showed excellent antifungal activities against P. infestans , with the EC₅₀value of 8.67 μg/mL, which were similar with that of dimethomorph (EC₅₀ value 8.34 μg/mL). Moreover, the target compounds exhibited certain antibacterial activities against Xanthomonas citri subsp. citri and Xanthomonas oryzae pv. oryzae.

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