School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
State Key Laboratory of Grassland Agro-ecosystems, Lanzhou University, Lanzhou 730000, China.
J Agric Food Chem. 2021 Dec 8;69(48):14467-14477. doi: 10.1021/acs.jafc.1c04242. Epub 2021 Nov 29.
Crop diseases caused by fungi threaten food security and exacerbate the food crisis. Inspired by the application of fungicide candidates from natural products in agrochemical discovery, a series of luotonin A derivatives were designed, synthesized, and evaluated for their antifungal activities against five plant fungi. Most of these compounds exhibited significant fungicidal activity against with EC values less than 1 μg/mL. Among them, compounds , , , and showed superior antifungal activity against with EC values of 0.036, 0.050, 0.042, and 0.048 μg/mL, respectively, which were more potent than boscalid (EC = 1.790 μg/mL). Preliminary mechanism studies revealed that compound might pursue its antifungal activity by disrupting the fungal cell membrane and cell wall. Moreover, bioassay also indicated that compound could be effective for the control of . The above results evidenced the potential of luotonin A derivatives as novel and promising candidate fungicides.
真菌引起的作物病害威胁着粮食安全，加剧了粮食危机。受农用杀菌剂候选物来源于天然产物在农业化学发现中的应用启发，设计、合成了一系列洛托菌素 A 衍生物，并对它们对五种植物真菌的抗真菌活性进行了评价。这些化合物大多数对 具有显著的杀菌活性，EC 值小于 1 μg/mL。其中，化合物 、 、 、 对 表现出优异的抗真菌活性，EC 值分别为 0.036、0.050、0.042 和 0.048 μg/mL，活性强于肟菌酯（EC = 1.790 μg/mL）。初步的机制研究表明，化合物 可能通过破坏真菌细胞膜和细胞壁来发挥其抗真菌活性。此外， 生物测定还表明，化合物 可有效防治 。上述结果证明了洛托菌素 A 衍生物作为新型有前途的候选杀菌剂的潜力。
