New thymol-derived triazole exhibits promising activity against Trichophyton rubrum

Fungal infections have emerged worldwide, and azole antifungals are widely used to control these infections. However, the emergence of antifungal resistance has been compromising the effectiveness of these drugs. Therefore, the objective of this study was to evaluate the antifungal and cytotoxic act...

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Veröffentlicht in:Brazilian journal of microbiology 2024-06, Vol.55 (2), p.1287-1295
Hauptverfasser: de Sousa Cutrim, Thiago Antonio, Eloy, Mariana Alves, Barcelos, Fernando Fontes, Meireles, Leandra Martins, de Freitas Ferreira, Lara Chaves, Reis, Tatiana Alves, Gonçalves, Sarah Santos, Lacerda, Valdemar, Fronza, Marcio, Morais, Pedro Alves Bezerra, Scherer, Rodrigo
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Sprache:eng
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Zusammenfassung:Fungal infections have emerged worldwide, and azole antifungals are widely used to control these infections. However, the emergence of antifungal resistance has been compromising the effectiveness of these drugs. Therefore, the objective of this study was to evaluate the antifungal and cytotoxic activities of the nine new 1,2,3 triazole compounds derived from thymol that were synthesized through Click chemistry. The binding mode prediction was carried out by docking studies using the crystallographic structure of Lanosterol 14α-demethylase G73E mutant from Saccharomyces cerevisiae . The new compounds showed potent antifungal activity against Trichophyton rubrum but did not show relevant action against Aspergillus fumigatus and Candida albicans . For T. rubrum , molecules nº 5 and 8 showed promising results, emphasizing nº 8, whose fungicidal and fungistatic effects were similar to fluconazole. In addition, molecule nº 8 showed low toxicity for keratinocytes and fibroblasts, concluding that this compound demonstrates promising characteristics for developing a new drug for dermatophytosis caused by T. rubrum , or serves as a structural basis for further research.
ISSN:1517-8382
1678-4405
1678-4405
DOI:10.1007/s42770-024-01295-0