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Molecules 2012, 17(5), 5882-5892; doi:10.3390/molecules17055882

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

1
Laboratório de Micologia Médica, Centro de Ciências Biológicas, Universidade Federal de Pernambuco (UFPE), 50670-901, Recife, PE, Brazil
2
Laboratório de Síntese Orgânica, Departamento de Química Fundamental, Universidade Federal de Pernambuco (UFPE), 50740-560, Recife, PE, Brazil
3
Laboratório de Síntese e Vetorização de Substâncias Bioativas, Universidade Estadual da Paraíba (UEPB), 58058-420, João Pessoa, PB, Brazil
4
Laboratório de Farmacologia Pré-Clínica e Toxicologia de Produtos Bioativos, Departamento de Fisiologia e Farmacologia, Universidade Federal de Pernambuco (UFPE), 50670-901, Recife, PE, Brazil
*
Author to whom correspondence should be addressed.
Received: 12 April 2012 / Revised: 3 May 2012 / Accepted: 5 May 2012 / Published: 16 May 2012
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Abstract

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.
Keywords: click chemistry; 1,2,3-triazoles; Candida spp.; antifungal activity click chemistry; 1,2,3-triazoles; Candida spp.; antifungal activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Lima-Neto, R.G.; Cavalcante, N.N.M.; Srivastava, R.M.; Mendonça Junior, F.J.B.; Wanderley, A.G.; Neves, R.P.; dos Anjos, J.V. Synthesis of 1,2,3-Triazole Derivatives and in Vitro Antifungal Evaluation on Candida Strains. Molecules 2012, 17, 5882-5892.

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