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

作　　者：Hui Tang Juan Wu Wen Zhang Lei Zhao Ya-Hui Zhang Cheng-Wu Shen 

机构地区：[1]Department of Pharmacy,Shandong Provincial Hospital Affiliated to Shandong University [2]Department of Pharmacy,General Hospital of PIA Chengdu Military Area Command

出　　处：《Chinese Chemical Letters》2015年第9期1161-1164,共4页中国化学快报（英文版）

基　　金：supported by the Shandong Natural Science Foundation(No.ZR2012HQ026);the Foundation of Sichuan Provincial Health Department(No.110480)

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.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.

关 键 词：Non-azole Biological evaluation Structure-activity relationships Synthesis Antifungal agents 

分 类 号：O626[理学—有机化学] TQ460.1[理学—化学]