Design, synthesis and biological evaluation of novel non-azole derivatives as potential antifungal agents

作者：Tang, Hui; Wu, Juan; Zhang, Wen; Zhao, Lei; Zhang, Ya-Hui; Shen, Cheng-Wu^*

来源：Chinese Chemical Letters, 2015, 26(9): 1161-1164.

DOI：10.1016/j.cclet.2015.04.030

• Non-azole
• Biological evaluation
• Structure-activity relationships
• Synthesis
• Antifungal agents

A series of 3-substituted quinazolinones, 2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro. The new compounds revealed excellent in vitro antifungal activity with broad spectrum. The structure-activity relationships (SARs) of the derivatives were analyzed. Compound 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole, especially against Trichophyton rubrum and Microsporum gypseum. This study provides a series of novel lead compounds for the development of non-azole antifungal agents.

• 出版日期2015-9
• 单位山东大学; 中国人民解放军总医院; 中国人民解放军成都军区总医院; 山东省立医院