Publication | Open Access
Synthesis of 1,2,3-Triazole Derivatives and in Vitro Antifungal Evaluation on Candida Strains
71
Citations
24
References
2012
Year
Bioorganic ChemistryAntimicrobial ChemotherapyClick ChemistryPharmaceutical ChemistryTen CompoundsMedicinal Chemistry1,2,3-Triazole DerivativesCandida StrainsAntifungal AgentsVitro Antifungal EvaluationAntimicrobial CompoundNatural Product SynthesisPharmacologyBiomolecular EngineeringAntifungal AgentNatural SciencesBetter Drug CandidateMedicineDrug Discovery
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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