4.6 Article

Synthesis of 1,2,3-Triazole Derivatives and in Vitro Antifungal Evaluation on Candida Strains

Journal

MOLECULES
Volume 17, Issue 5, Pages 5882-5892

Publisher

MDPI
DOI: 10.3390/molecules17055882

Keywords

click chemistry; 1,2,3-triazoles; Candida spp.; antifungal activity

Funding

  1. CAPES
  2. CNPq
  3. PPP/FACEPE
  4. PRONEX/FACEPE

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1,2,3-Triazoles have been extensively studied as compounds possessing important biological activities. In this work, we describe the synthesis of ten 2-(1-aryl-1H-1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or click chemistry). Next the in vitro antifungal activity of these ten compounds was evaluated using the microdilution broth method against 42 isolates of four different Candida species. Among all tested compounds, the halogen substituted triazole 2-[1-(4-chlorophenyl)-1H-(1,2,3)triazol-4-yl]propan-2-ol, revealed the best antifungal profile, showing that further modifications could be done in the structure to obtain a better drug candidate in the future.

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