标题：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
作者机构：[Tang, H] Department of Pharmacy, Shandong Provincial Hospital, Shandong University, Jinan, 250021, China;[ Wu, J] Department of Pharmacy, General Hos 更多
通讯作者地址：[Shen, CW]Shandong Univ, Shandong Prov Hosp, Dept Pharm, Jinan 250021, Peoples R China.
关键词：Non-azole; Biological evaluation; Structure-activity relationships;; Synthesis; Antifungal agents
摘要：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. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved.