摘要/Abstract

合成了一系列含有1，3，4-噁二唑的杨梅素衍生物，所有化合物经¹H NMR，¹³C NMR以及HRMS表征.生物活性测试表明，部分化合物对柑橘溃疡病菌（Xac）、水稻白叶枯病菌（Xoo）以及烟草花叶病病毒（TMV）具有较好的抑制作用.其中化合物4a、4b、4f、4j对柑橘溃疡病菌的EC₅₀分别为18.5、40.7、26.9和32.4 μg/mL，优于对照药叶枯唑（68.8 μg/mL）·化合物4f、4j对水稻白叶枯的EC₅₀分别为45.9和35.7 μg/mL，优于对照药叶枯唑（69.3 μg/mL）·对TMV治疗活性，化合物4n的EC₅₀值为272.8 μg/mL，优于对照药宁南霉素（428.8 μg/mL）·对TMV保护活性，化合物4f的EC₅₀值为235.6 μg/mL，优于对照药宁南霉素（447.9 μg/mL）.化合物4j与南方水稻黑条矮缩病毒P9-1作用的微量热涌动实验表明，该化合物与P9-1之间具有较强的相互作用.
关键词: 杨梅素, 噁二唑, 生物活性, 蛋白
A series of novel myricetin derivatives containing 1,3,4-oxadiazole moiety were designed and synthesized.Bioassays indicated that some compounds showed potential antibacterial and antiviral activities. Among them, compounds 4a,4b, 4f and 4j demonstrated appreciable inhibitory effect against Xanthomonas axonopodis pv.citri (Xac), with half-maximal effective concentration (EC₅₀) values of 18.5, 40.7, 26.9 and 32.4 μg/mL, which were significantly better than commercial agent bismerthiazol (68.8 μg/mL), compounds 4f and 4j also demonstrated appreciable inhibitory effect against Xanthomonas oryzae pv. Oryzae (Xoo) with EC₅₀ values of 45.9 and 35.7 μg/mL, which were better than commercial agent bismerthiazol (69.3 μg/mL). In addition, compounds 4n demonstrated significant curative activity against TMV with EC₅₀ value of 272.8 μg/mL, which was better than commercial agent ningnamycin (428.8 μg/mL), compounds 4f showed protecting activity against tobacco mosaic virus (TMV) with EC₅₀ value of 235.6 μg/mL, which was better than commercial agent ningnamycin (447.9 μg/mL). Microscale thermophoresis (MST) indicated that compound 4j could bind with south rice black drawf virus P9-1.
Key words: myricetin, oxadiazole, biological activity, protein


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