Citation: Hui Tang, Juan Wu, Wen Zhang, Lei Zhao, Ya-Hui Zhang, Cheng-Wu Shen. Design, synthesis and biological evaluation of novel non-azole derivatives as potential antifungal agents[J]. Chinese Chemical Letters, ;2015, 26(9): 1161-1164. doi: 10.1016/j.cclet.2015.04.030 shu

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

Hui Tang ¹ ,
Juan Wu ² ,
Wen Zhang ¹ ,
Lei Zhao ¹ ,
Ya-Hui Zhang ¹ ,
Cheng-Wu Shen ^1,,

1.
1 Department of Pharmacy, Shandong Provincial Hospital Affiliated to Shandong University, Jinan 250021, China;
2.
2 Department of Pharmacy, General Hospital of PLA Chengdu Military Area Command, Chengdu 610083, China

Corresponding author: Cheng-Wu Shen,
Received Date: 5 January 2015
Available Online: 3 April 2015
Fund Project: the Foundation of Sichuan Provincial Health Department (No. 110480). (No. ZR2012HQ026)

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.
- Non-azole,
- Biological evaluation,
- Structure-activity relationships,
- Synthesis,
- Antifungal agents
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