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

Molecules

Reginaldo G. Lima-Neto¹  Nery N. M. Cavalcante¹  Rajendra M. Srivastava¹  Francisco J. B. Mendonça Junior¹  Almir G. Wanderley¹  Rejane P. Neves¹ 

[1] ¹Laboratório de Micologia Médica, Centro de Ciências Biológicas, Universidade Federal de Pernambuco (UFPE), 50670-901, Recife, PE, Brazil

关键词: click chemistry;    1;    2;    3-triazoles;    Candida spp.;    antifungal activity;   

DOI  :  10.3390/molecules17055882

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.