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Merck

Synthesis of 1,2,3-triazole derivatives and in vitro antifungal evaluation on Candida strains.

Molecules (Basel, Switzerland) (2012-05-18)
Reginaldo G Lima-Neto, Nery N M Cavalcante, Rajendra M Srivastava, Francisco J B Mendonça Junior, Almir G Wanderley, Rejane P Neves, Janaína V dos Anjos
RESUMEN

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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Sigma-Aldrich
(±)-Miconazole nitrate salt, imidazole antibiotic
Supelco
(±)-Miconazole nitrate salt, Pharmaceutical Secondary Standard; Certified Reference Material
Miconazole nitrate, European Pharmacopoeia (EP) Reference Standard
Miconazole, European Pharmacopoeia (EP) Reference Standard