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二氢香芹酮杂化衍生物对……的体外抗真菌活性及毒性

In Vitro Antifungal Activity and Toxicity of Dihydrocarvone-Hybrid Derivatives against .

作者信息

Díaz Katy, Werner Enrique, Besoain Ximena, Flores Susana, Donoso Viviana, Said Bastian, Caro Nelson, Vega Ernesto, Montenegro Iván, Madrid Alejandro

机构信息

Departamento de Química, Universidad Técnica Federico Santa María, Av. España N° 1680, Valparaíso 2340000, Chile.

Departamento de Ciencias Básicas, Campus Fernando May, Universidad del Bío-Bío, Avda. Andrés Bello 720, Casilla 447, Chillán 3780000, Chile.

出版信息

Antibiotics (Basel). 2021 Jul 6;10(7):818. doi: 10.3390/antibiotics10070818.

Abstract

The aim of this study was to synthesize a series of novel and known dihydrocarvone-hybrid derivatives (-) and to evaluate mycelial growth activity of hybrid molecules against two strains of , as well as their toxicity. Dihydrocarvone-hybrid derivatives have been synthesized under sonication conditions and characterized by FTIR, NMR, and HRMS. Antifungal efficacy against both strains of was determined by half maximal effective concentration (EC) and toxicity using the brine shrimp lethality test (BSLT). Among the synthesized compounds, and showed the best activity against both strains of with EC values of 148.1 and 145.9 µg/mL for strain 1 and 18.1 and 15.7 µg/mL for strain 2, respectively, compared to BC 1000 (commercial organic fungicide) but lower than Mystic 520 SC. However, these compounds showed low toxicity values, 910 and 890 µg/mL, respectively, compared to Mystic 520 SC, which was highly toxic. Based on the results, these hybrid compounds could be considered for the development of more active, less toxic, and environmentally friendly antifungal agents against phytopathogenic fungi.

摘要

本研究的目的是合成一系列新型和已知的二氢香芹酮杂化衍生物(-),并评估杂化分子对两种菌株的菌丝生长活性及其毒性。二氢香芹酮杂化衍生物已在超声条件下合成,并通过傅里叶变换红外光谱(FTIR)、核磁共振(NMR)和高分辨率质谱(HRMS)进行表征。通过半数有效浓度(EC)测定对两种菌株的抗真菌效力,并使用卤虫致死试验(BSLT)测定其毒性。在合成的化合物中,[具体化合物名称1]和[具体化合物名称2]对两种菌株均表现出最佳活性,菌株1的EC值分别为148.1和145.9 µg/mL,菌株2的EC值分别为18.1和15.7 µg/mL,与BC 1000(商业有机杀菌剂)相比,但低于Mystic 520 SC。然而,与高毒性的Mystic 520 SC相比,这些化合物的毒性值较低,分别为910和890 µg/mL。基于这些结果,这些杂化化合物可被考虑用于开发针对植物病原真菌的活性更高、毒性更低且环境友好的抗真菌剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc88/8300761/dfbed834dded/antibiotics-10-00818-sch001.jpg

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