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

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-1 H -1,2,3-triazol-4-yl)propan-2-ols via copper catalyzed azide alkyne cycloaddition (CuAAc or click chemistry ). Next the in vitro antifung...

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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2012-05, Vol.17 (5), p.5882-5892
Hauptverfasser: Almir G. Wanderley, Janaína V. dos Anjos, Rejane P. Neves, Francisco J. B. Mendonça Junior, Rajendra M. Srivastava, Nery N. M. Cavalcante, Reginaldo G. Lima-Neto
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Sprache:eng
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Zusammenfassung: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-1 H -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)-1 H -(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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules17055882