Innovation Center of Pesticide Research, Department of Applied Chemistry, China Agricultural University, Beijing 100193, China.
Molecules. 2022 Aug 17;27(16):5259. doi: 10.3390/molecules27165259.
In order to overcome the resistance of phytopathogens to commercial fungicides, a series of optical 2-methyl-2,3-diol-5-pentyl-based cinnamamide derivatives were rationally designed, synthesized, characterized, and evaluated for their in vitro and in vivo fungicidal activities. The bioassay results indicated that the EC (concentration for 50% of maximal effect) values of ()-, ()-, ()- and ()- were 0.16, 0.28, 0.41 and 0.47 µg/mL in the in vitro evaluation against , respectively, while compounds ()- and ()-, ()- and ()- exhibited excellent in vivo fungicidal activity against with inhibition rates of 100% at 400 μg/mL. These findings supported the idea that optical 2-methyl-2,3-diol-5-pentyl-containing cinnamamides ()- and ()-, ()- and ()- with 2-chloro-4-trifluoromethyl aniline and 2-(4-chlorophenyl) aniline showed excellent in vivo fungicidal activity against and and were promising fungicide candidates.
为了克服植物病原菌对商业杀菌剂的抗性，我们合理设计、合成、表征了一系列光学 2-甲基-2,3-二醇-5-戊基肉桂酰胺衍生物，并评估了它们的体外和体内杀菌活性。生物测定结果表明，在体外评估中，()-、()-、()-和()-对 的 EC（最大效应 50%的浓度）值分别为 0.16、0.28、0.41 和 0.47 µg/mL，而化合物()-和()-、()-和()-对 的体内杀菌活性优异，在 400 µg/mL 时抑制率均为 100%。这些发现支持了这样的观点，即光学 2-甲基-2,3-二醇-5-戊基含肉桂酰胺（）-和（）-、（）-和（）-与 2-氯-4-三氟甲基苯胺和 2-（4-氯苯基）苯胺具有出色的体内杀菌活性，对 和 表现出优异的防治效果，是有前途的杀菌剂候选物。
