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4‐Aminoquinolines Bearing a 1,3‐Benzodioxole Moiety: Synthesis and Biological Evaluation as Potential Antifungal Agents
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2021-03-24 , DOI: 10.1002/cbdv.202100106 Rui Yang 1 , Zhuolin Li 1 , Jialing Xie 1 , Jianchuan Liu 1 , Tianhong Qin 1 , Junda Liu 1 , Haiying Du 2 , Haoyun Ye 1
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2021-03-24 , DOI: 10.1002/cbdv.202100106 Rui Yang 1 , Zhuolin Li 1 , Jialing Xie 1 , Jianchuan Liu 1 , Tianhong Qin 1 , Junda Liu 1 , Haiying Du 2 , Haoyun Ye 1
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In search of new environmentally friendly and effective antifungal agents, a series of 4‐aminoquinolines bearing a 1,3‐benzodioxole moiety were prepared and their structures were fully elucidated by spectroscopic analyses. The antifungal activities of all the target compounds against five phytopathogenic fungi were evaluated in vitro. The results revealed that most of the newly synthesized compounds exhibited obvious inhibitory activities at the concentration of 50 μg/mL. Among them, 6‐(furan‐2‐yl)‐N‐(4‐methylphenyl)‐2H‐[1,3]dioxolo[4,5‐g]quinolin‐8‐amine hydrochloride (7m) displayed more promising antifungal potency with EC50 values of 10.3 and 14.0 μg/mL against C. lunata and A. alternate, respectively. Particularly, the EC50 value of 7m against C. lunata was 7.3‐fold as potent as the standard azoxystrobin. There were some significant morphological alterations in the mycelia of C. lunata when treated with 7m at 50 μg/mL. Additionally, the preliminary structure–activity relationships (SARs) were also discussed. Thus, this study suggests that 4‐aminoquinolines bearing a 1,3‐benzodioxole moiety are interesting scaffolds for the development of novel antifungal agents.
中文翻译：
带有 1,3-苯并二氧杂环戊烷部分的 4-氨基喹啉：作为潜在抗真菌剂的合成和生物学评价
为了寻找新的环境友好且有效的抗真菌剂，制备了一系列带有 1,3-苯并二氧杂环戊二烯部分的 4-氨基喹啉，并通过光谱分析充分阐明了它们的结构。体外评价了所有目标化合物对五种植物病原真菌的抗真菌活性。结果表明，大多数新合成的化合物在50 μg/mL的浓度下表现出明显的抑制活性。其中，6-（呋喃-2-基） - ñ - （4-甲基苯基）-2 ħ - [1,3]二氧杂环戊烯并[4,5-克]喹啉-8-胺盐酸盐（7米）显示更有前途的抗真菌EC 50值为 10.3 和 14.0 μg/mL 的效力C. lunata和A.分别是交替的。特别是，7m的 EC 50值对C. lunata 的效力是标准嘧菌酯的 7.3 倍。当用50 μg/mL 的7m处理时，C. lunata的菌丝体有一些显着的形态学改变。此外，还讨论了初步的构效关系 (SAR)。因此，这项研究表明，带有 1,3-苯并二氧杂环戊烯部分的 4-氨基喹啉是开发新型抗真菌剂的有趣支架。
更新日期：2021-05-17
中文翻译：
带有 1,3-苯并二氧杂环戊烷部分的 4-氨基喹啉：作为潜在抗真菌剂的合成和生物学评价
为了寻找新的环境友好且有效的抗真菌剂，制备了一系列带有 1,3-苯并二氧杂环戊二烯部分的 4-氨基喹啉，并通过光谱分析充分阐明了它们的结构。体外评价了所有目标化合物对五种植物病原真菌的抗真菌活性。结果表明，大多数新合成的化合物在50 μg/mL的浓度下表现出明显的抑制活性。其中，6-（呋喃-2-基） - ñ - （4-甲基苯基）-2 ħ - [1,3]二氧杂环戊烯并[4,5-克]喹啉-8-胺盐酸盐（7米）显示更有前途的抗真菌EC 50值为 10.3 和 14.0 μg/mL 的效力C. lunata和A.分别是交替的。特别是，7m的 EC 50值对C. lunata 的效力是标准嘧菌酯的 7.3 倍。当用50 μg/mL 的7m处理时，C. lunata的菌丝体有一些显着的形态学改变。此外，还讨论了初步的构效关系 (SAR)。因此，这项研究表明，带有 1,3-苯并二氧杂环戊烯部分的 4-氨基喹啉是开发新型抗真菌剂的有趣支架。
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