Felippe William Q, Barbosa Igor R, Oliveira Aguida A, da Costa Gisela L, Echevarria Aurea
Institute of Chemistry, Federal Rural University of Rio de Janeiro, BR 465, km 7, Seropedica, RJ, Brazil.
Institute of Veterinary, Federal Rural University of Rio de Janeiro, BR 465, km 7, Seropedica, RJ, Brazil.
Arch Microbiol. 2025 Jan 4;207(1):24. doi: 10.1007/s00203-024-04229-4.
The frequency of opportunistic fungal infections has been increasing, impacting agriculture, food, and health sectors. In this work, four thiosemicarbazone-chalcones (TC) were synthesized and evaluated by the radial diffusion method against filamentous fungi. All TCs were effective against Aspergillus parasiticus, especially the fluor-substituted one, with radial growth inhibition of 62,9% and 74,4% at the lower (0.209 µmol/ml) and highest (1.670 µmol/ml) concentrations tested, respectively. On the other hand, the non-substituted derivative was the most active against A. carbonarius, inhibiting radial growth by 47,9% and 74,1% at 0.222 µmol/ml and 1.777 µmol/ml, respectively. Additionally, the compounds were evaluated against the dimorphic fungi Sporothrix brasiliensis, S. schenckii, and a clinical strain of Sporothrix spp, exhibiting minimum inhibitory concentrations (MICs) in the range of 0.396-1.777 µmol/ml. When tested against four yeasts of the Candida genus, the thiosemicarbazone-chalcones demonstrated greater activity against C. krusei (MICs 0.011-0.026 µmol/ml).
机会性真菌感染的频率一直在增加，影响着农业、食品和卫生部门。在这项工作中，合成了四种硫代氨基脲-查耳酮（TC），并通过径向扩散法对丝状真菌进行了评估。所有的TC对寄生曲霉都有效，尤其是氟取代的那种，在测试的较低浓度（0.209微摩尔/毫升）和最高浓度（1.670微摩尔/毫升）下，径向生长抑制率分别为62.9%和74.4%。另一方面，未取代的衍生物对黑曲霉最具活性，在0.222微摩尔/毫升和1.777微摩尔/毫升时，分别抑制径向生长47.9%和74.1%。此外，还对这些化合物针对双态真菌巴西孢子丝菌、申克孢子丝菌和一株临床孢子丝菌属菌株进行了评估，其最低抑菌浓度（MIC）在0.396 - 1.777微摩尔/毫升范围内。当针对念珠菌属的四种酵母进行测试时，硫代氨基脲-查耳酮对克鲁斯念珠菌表现出更大的活性（MIC为0.011 - 0.026微摩尔/毫升）。
