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Cinnamyl Schiff bases: synthesis, cytotoxic effects and antifungal activity of clinical interest
Letters in Applied Microbiology ( IF 2.0 ) Pub Date : 2020-08-10 , DOI: 10.1111/lam.13356
T F F Magalhães 1 , C M da Silva 2 , L B F Dos Santos 2 , D A Santos 1 , L M Silva 3 , B B Fuchs 4 , E Mylonakis 4 , C V B Martins 5 , M A de Resende-Stoianoff 1 , Â de Fátima 2
Affiliation  

The aim of this study was to synthesize and investigate the in vitro antifungal properties of 23 cinnamyl Schiff bases. In addition, cytotoxic effects of such cinnamyl Schiff bases against human lung, kidney or red blood cells were also checked. The compounds were synthesized in a single‐step, 2 min of reaction under microwave irradiation produced up to 97% yield. Six of the 23 cinnamyl Schiff bases possessed antifungal activities against strains of Candida, Aspergillus, Fonsecaea and, particularly, Cryptococcus species. Indeed, cinnamyl Schiff bases 1 and 23 exhibited minimum inhibitory concentration (MIC) values more than twofold lower than fluconazole (FCZ) against all the Cryptococcus neoformans strains (MIC = 1·33, 1·4 and 5·2 µg ml−1, respectively) and Cryptococcus gattii strains (MIC = 5·3, 2·8 and 9·2 µg ml−1, respectively) (12 strains of each species) while cinnamyl Schiff base 11 was as potent as FCZ against all strains from both Cryptococcus species. No significant cytotoxic effects were observed for Schiff bases against human lung, kidney or red blood cells, all presenting selective indexes higher than 10. In conclusion, this study revealed cinnamyl Schiff bases, especially 1 and 23, as new lead anticryptococcal agents for the discovery of novel antifungal drugs.

中文翻译:

肉桂基席夫碱:具有临床意义的合成、细胞毒作用和抗真菌活性

本研究的目的是合成和研究 23 种肉桂基席夫碱的体外抗真菌特性。此外,还检查了此类肉桂基席夫碱对人肺、肾或红细胞的细胞毒性作用。这些化合物是一步合成的,在微波辐射下反应 2 分钟,产率高达 97%。23 种肉桂基席夫碱中的 6 种对念珠菌属、曲霉属、Fonsecaea 和特别是隐球菌属具有抗真菌活性。事实上,肉桂基席夫碱 1 和 23 对所有新型隐球菌菌株(MIC = 1·33、1·4 和 5·2 µg ml-1,分别)和 Cryptococcus gattii 菌株(MIC = 5·3、2·8 和 9·2 µg ml-1,分别)(每个物种 12 个菌株),而肉桂基席夫碱 11 与 FCZ 一样有效对抗来自两种隐球菌物种的所有菌株。没有观察到希夫碱对人肺、肾或红细胞的显着细胞毒性作用,所有选择指数都高于 10。 总之,这项研究揭示了肉桂基希夫碱,尤其是 1 和 23,作为新的先导抗隐球菌药物发现新型抗真菌药物。
更新日期:2020-08-10
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