Citation: Xu Yuan-Yuan, Qian An-Ran, Cao Xu-Feng, Ling Chen-Yu, Cao Yong-Bing, Wang Rui-Lian, Li Yi-Su, Yang Yu-She. Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents[J]. Chinese Chemical Letters, ;2016, 27(5): 703-706. doi: 10.1016/j.cclet.2016.01.040 shu

Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents

a.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China
b.
School of Pharmacy, Second Military Medical University, Shanghai 200433, China
c.
Drug Discovery and Design Center, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China

Corresponding author: Yang Yu-She, ysyang@simm.ac.cn
Received Date: 6 August 2015
Revised Date: 4 November 2015
Accepted Date: 14 January 2016
Available Online: 1 May 2016

Figures(5)

A series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by ¹H NMR, ¹³C NMR and HRMS. The in vitro antifungal activities of the target compounds were evaluated. The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.
- Synthesis,
- Triazole,
- γ-Lactam,
- Antifungal activity
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1.
沈阳化工大学材料科学与工程学院沈阳 110142