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Design, synthesis, and in vitro antifungal evaluation of novel triazole derivatives bearing alkynyl side chains
Joint Authors
Wang, Ting
Cai, Zhangyong
Jiang, Yuanying
Zhang, Dazhi
Ni, Tingjunhong
Pang, Lei
Xie, Fei
Ding, Zichao
Hao, Yumeng
Yu, Shichong
Chai, Xiaoyun
Jin, Yongsheng
Li, Ran
Source
Journal of Saudi Chemical Society
Issue
Vol. 23, Issue 5 (31 Jul. 2019), pp.576-585, 10 p.
Publisher
Publication Date
2019-07-31
Country of Publication
Saudi Arabia
No. of Pages
10
Main Subjects
Topics
Abstract EN
In order to explore novel antifungal agents, twenty-seven triazole derivatives featuring an alkyne linker in the side chain were designed and synthesized by the Sonogashira reaction.
Most of the target compounds exhibited good antifungal activity against eight human pathogenic fungi, especially excellent activity against Candida and Cryptococcus species, comparing with the reference drugs fluconazole, voriconazole and ravuconazole.
Compounds A2 and A3 exhibited in vitro activity against all the tested fungi with MIC80 values ranging from 0.0156 μg/mL to 0.5 μg/mL, which are superior to ravuconazole and fluconazole.
SAR and molecular docking study give a clear conclusion that para-fluoro, para-chloro, and para-cyano substituted phenylalkynyl or pyridinylalkynyl side chains may promote triazole antifungal activity.
American Psychological Association (APA)
Ni, Tingjunhong& Pang, Lei& Cai, Zhangyong& Xie, Fei& Ding, Zichao& Hao, Yumeng…[et al.]. 2019. Design, synthesis, and in vitro antifungal evaluation of novel triazole derivatives bearing alkynyl side chains. Journal of Saudi Chemical Society،Vol. 23, no. 5, pp.576-585.
https://search.emarefa.net/detail/BIM-889258
Modern Language Association (MLA)
Ni, Tingjunhong…[et al.]. Design, synthesis, and in vitro antifungal evaluation of novel triazole derivatives bearing alkynyl side chains. Journal of Saudi Chemical Society Vol. 23, no. 5 (Jul. 2019), pp.576-585.
https://search.emarefa.net/detail/BIM-889258
American Medical Association (AMA)
Ni, Tingjunhong& Pang, Lei& Cai, Zhangyong& Xie, Fei& Ding, Zichao& Hao, Yumeng…[et al.]. Design, synthesis, and in vitro antifungal evaluation of novel triazole derivatives bearing alkynyl side chains. Journal of Saudi Chemical Society. 2019. Vol. 23, no. 5, pp.576-585.
https://search.emarefa.net/detail/BIM-889258
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references : p. 584-585
Record ID
BIM-889258