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

• 作 者: Yuan-Yuan Xu An-Ran Qian Xu-Feng Cao Chen-Yu Ling Yong-Bing Cao Rui-Lian Wang Yi-Su Li Yu-She Yang
• 机 构: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for
• 出 处: Chinese Chemical Letters
• 发表日期: 2016年05期
• 关键词: antifungal lactam triazole fungi Candida potent solubility stronger clinically t

A series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by ~1H NMR,~(13)CNMR 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.

The series of novel triazole derivatives containing γ-lactam were designed and synthesized, and their structures were confirmed by ~ 1H NMR, ~ (13) CNMR and HRMS. The in vitro antifungal activities of the target compounds were as. of the compounds for 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.