Abstract

Series of thioether derivatives containing 4-methylumbelliferone fused oxazole moiety were designed and synthesised, their structures were fully characterized by ¹H NMR, ¹³C NMR and HR-ESI-MS as well. Moreover, the in vitro antifungal potency of the title compounds were preliminarily evaluated for their possible use as a fungicide. Meanwhile, ethyl thioethers 3aa and 3ba displayed remarkable inhibitory effect against the mycelium growth of Valsa mali and Botrytis cinerea with EC₅₀ of 12–16 μg/mL. Furthermore, compounds 3aa and 3ba also exhibited > 88% protective and curative effect against B. cinerea on tomato fruits at 90 μg/mL. Additionally, the environmental toxicity of the title compounds against the brine shrimp Artemia salina were evaluated as well. The results indicated that most of the title compounds exhibited weak toxic to aquatic organism A. salina.

摘要

设计合成了一系列含4-甲基伞形酮稠合恶唑的硫醚衍生物，并通过¹ H NMR、¹³ C NMR和HR-ESI-MS对其结构进行了全面表征。此外，对标题化合物的体外抗真菌效力进行了初步评估，以确定它们可能用作杀真菌剂。同时，乙基硫醚3aa和3ba对Valsa mali和Botrytis cinerea的菌丝体生长具有显着的抑制作用，EC ₅₀为 12-16 μg/mL。此外，化合物3aa和3ba在 90 μg/mL 的番茄果实上也表现出 > 88% 的对B. cinerea的保护和治疗作用。此外，还评估了标题化合物对盐水虾卤虫的环境毒性。结果表明，大多数标题化合物对水生生物A. salina 具有弱毒性。