期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 45, 期 10, 页码 4435-4445出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2010.07.002
关键词
Triazole; Synthesis; Click reaction; Antifungal activity; CYP51
资金
- National Natural Science Foundation of China [20772153]
- Eleventh Five Year Military Medicine [06MB206]
- Shanghai Leading Academic Discipline Project [B906]
A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols (1a-v, 2a-w), which are analogues of fluconazole. have been designed and synthesized as the potential antifungal agents by the click reaction. Click reaction approach toward the synthesis of two sets of novel 12,3-triazolyl linked triazole antifungal derivatives 1a-v, 2a-w was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of propargylated intermediate 8 with substituted azidomethyl benzene. The 1,2,3-triazolyl group was inserted into the side chain of the target molecule which can increase the antifungal activity of compounds. (C) 2010 Elsevier Masson SAS All rights reserved.
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