Tang Chenghao, Guo Wenbo, Yang Shengzhou, Hu Xiuhong, Chen Xingju, Wang Xiang
School of Life and Health Science, Kaili University, Kaili, China.
Front Chem. 2023 Jul 20;11:1233443. doi: 10.3389/fchem.2023.1233443. eCollection 2023.
A series of 1,4-benzoxazin-3-one derivatives containing an acylhydrazone moiety were designed, synthesized and evaluated for their antifungal activities against , , , , and . The structures of target compounds were characterized by H NMR, H NMR, F NMR and HRMS. The preliminary antifungal evaluation of all target compounds showed that some target compounds possessed moderate to good activities against , , and . Among them, compounds and exhibited noticeable inhibition effects against with the EC values (effective concentration for 50% activity) of 20.06 and 23.17 g/ml, respectively, which were even nearly double effective than that of hymexazol (40.51 g/ml). Meanwhile, compound displayed a notable inhibitory effect toward , with the EC value of 26.66 μg/ml, which was better than that of hymexazol (32.77 g/ml). In addition, compound yielded the EC value of 15.37 g/ml against , which was less than those of hymexazol (18.35 g/ml) and carbendazim (34.41 g/ml). Eventually, compound showed higher inhibitory effect against , with EC value of 26.76 g/ml, which was better than that of hymexazol (>50 g/ml).
设计、合成了一系列含有酰腙部分的1,4 - 苯并恶嗪 - 3 - 酮衍生物，并对其针对[此处未明确列出的多种真菌名称]的抗真菌活性进行了评估。通过氢核磁共振（¹H NMR）、氢核磁共振（¹H NMR）、氟核磁共振（¹⁹F NMR）和高分辨质谱（HRMS）对目标化合物的结构进行了表征。所有目标化合物的初步抗真菌评估表明，一些目标化合物对[此处未明确列出的多种真菌名称]具有中度至良好的活性。其中，化合物[此处未明确列出化合物编号]和[此处未明确列出化合物编号]对[此处未明确列出的某种真菌名称]表现出显著的抑制作用，其半数有效浓度（EC值）分别为20.06和23.17μg/ml，甚至比恶霉灵（40.51μg/ml）的效果几乎高出一倍。同时，化合物[此处未明确列出化合物编号]对[此处未明确列出的某种真菌名称]表现出显著的抑制作用，EC值为26.66μg/ml，优于恶霉灵（32.77μg/ml）。此外，化合物[此处未明确列出化合物编号]对[此处未明确列出的某种真菌名称]的EC值为15.37μg/ml，低于恶霉灵（18.35μg/ml）和多菌灵（34. 41μg/ml）。最终，化合物[此处未明确列出化合物编号]对[此处未明确列出的某种真菌名称]表现出更高的抑制作用，EC值为26.76μg/ml，优于恶霉灵（>50μg/ml）。
