在我国最重要的水产养殖资源中，鲑鱼和鳟鱼脱颖而出。近几十年来，它们的产量显着增加，使其成为经济上最有价值的两种资源。然而，水产养殖的高产量导致许多病原体繁殖，导致传染病和重大生产损失。鲑鱼鱼立克次体是一种革兰氏阴性、兼性细胞内细菌，可引起多种鲑科鱼类的严重疾病。尽管鲑鱼对水产养殖产生重大影响，但对该疾病的有效治疗方法仍然有限。目前的预防和控制策略通常包括抗生素和疫苗。然而，这些治疗方法显示出不同程度的疗效。一种有前途的方法涉及合成具有抗菌特性的生物活性类似化合物。醌类是自然界中丰富的次级代谢产物，由于其多种生理活性（包括抗生素、杀虫、抗真菌和抗癌特性）而成为人们关注的焦点。在这项研究中，展示了 6-溴-7-芳基氨基异喹啉-5,8-醌系列的合成，并使用经典光谱方法（如一维核磁共振 (NMR)、FT-IR）对这些化合物进行了表征。红外）、质谱分析以及针对鲑鱼鱼立克次体的生物活性。溴化衍生化合物在任何评估浓度下均未表现出细胞毒性。此外，用类似化合物处理后鲑鱼的感染性表明衍生物甲基 6-溴-7-((4-甲氧基苯基)氨基)-1,3-二甲基-5,8-二氧代-5,8-二氢异喹啉-4-羧酸酯(4b)和甲基7-((4'-氨基-[1,1'-联苯]-4-基)氨基)-6-溴-1,3-二甲基-5,8-二氧代- 5,8-二氢异喹啉-4-羧酸盐 (4g) 在 25 μg/mL 浓度下可减少细菌负荷。© 2024 John Wiley

Among the most important aquaculture resources for our country, salmon and trout stand out. Their production has increased significantly in recent decades, making them two of the most valuable resources in economic terms. However, high aquaculture production has allowed many pathogens to proliferate, causing infectious diseases and significant production losses. Piscirickettsia salmonis is a gram-negative, facultative intracellular bacterium that is responsible for causing severe disease in a variety of salmonid fish species. Despite the significant impact of P. salmonis on aquaculture, effective treatments for this disease remain limited. Current prevention and control strategies often include antibiotics and vaccines. However, these treatments have shown varying degrees of efficacy. A promising approach involves synthesizing bioactive analog compounds with antibacterial properties. Quinones, secondary metabolites that are abundant in nature, have become a focal point of interest due to their diverse physiological activities, including antibiotic, insecticidal, antifungal, and anticancer properties. In this study, it is shown the synthesis of series 6-bromo-7-arylaminoisoquinoline-5,8-quinones, the characterization of these compounds using classical spectroscopic methods such as one-dimensional nuclear magnetic resonance (NMR), FT-IR (infrared), mass spectrometry, and the biological activity against Piscirickettsia salmonis. The brominated derivative compounds showed no cytotoxicity at any concentration evaluated. Furthermore, the infectivity of P. salmonis after treatment with the analog compounds indicated that derivatives methyl 6-bromo-7-((4-methoxyphenyl)amino)-1,3-dimethy-5,8-dioxo-5,8-dihydroisoquinoline-4-carboxylate (4b) and methyl 7-((4'-amino-[1,1'-biphenyl]-4-yl)amino)-6-bromo-1,3-dimethy-5,8-dioxo-5,8-dihydroisoquinoline-4-carboxylate (4g) reduced the bacterial load at 25 μg/mL concentration.© 2024 John Wiley & Sons Ltd.