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Braz J Microbiol ; 55(2): 1287-1295, 2024 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-38453819

RESUMEN

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.


Asunto(s)
Antifúngicos , Arthrodermataceae , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Timol , Triazoles , Antifúngicos/farmacología , Antifúngicos/química , Triazoles/farmacología , Triazoles/química , Humanos , Timol/farmacología , Timol/química , Arthrodermataceae/efectos de los fármacos , Arthrodermataceae/genética , Candida albicans/efectos de los fármacos , Candida albicans/genética , Aspergillus fumigatus/efectos de los fármacos , Aspergillus fumigatus/genética , Saccharomyces cerevisiae/efectos de los fármacos , Saccharomyces cerevisiae/genética , Queratinocitos/efectos de los fármacos , Trichophyton/efectos de los fármacos , Trichophyton/genética
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