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

被引:66
|
作者
Lima-Neto, Reginaldo G. [2 ]
Cavalcante, Nery N. M. [1 ]
Srivastava, Rajendra M. [1 ]
Mendonca Junior, Francisco J. B. [3 ]
Wanderley, Almir G. [4 ]
Neves, Rejane P. [2 ]
dos Anjos, Janaina V. [1 ]
机构
[1] Univ Fed Pernambuco UFPE, Dept Quim Fundamental, Lab Sintese Organ, BR-50740560 Recife, PE, Brazil
[2] Univ Fed Pernambuco UFPE, Ctr Ciencias Biol, Lab Micol Med, BR-50670901 Recife, PE, Brazil
[3] Univ Estadual Paraiba UEPB, Lab Sintese & Vetorizacao Subst Bioat, BR-58058420 Joao Pessoa, Paraiba, Brazil
[4] Univ Fed Pernambuco UFPE, Dept Fisiol & Farmacol, Lab Farmacol Preclin & Toxicol Prod Bioat, BR-50670901 Recife, PE, Brazil
来源
MOLECULES | 2012年 / 17卷 / 05期
关键词
click chemistry; 1,2,3-triazoles; Candida spp; antifungal activity; EFFICIENT SYNTHESIS; TRIAZOLE; INHIBITORS; SCHIFF;
D O I
10.3390/molecules17055882
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
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.
引用
收藏
页码:5882 / 5892
页数:11
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