Synthesis and Antifungal Activity of Some 6-tert-butyl-8-chloro-2, 3-dimethylquinolin-4-ol Derivatives against Pyricularia oryae

Author(s): Yue-Ming Fang, Rui-Rui Zhang, Zhong-Hua Shen, Cheng-Xia Tan, Jian-Quan Weng, Tian-Ming Xu*, Xing-Hai Liu*, Hong-Ying Huang, Hong-Ke Wu

Journal Name: Letters in Drug Design & Discovery

Volume 15 , Issue 12 , 2018

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Graphical Abstract:


Background: A series of new 6-(tert-butyl)-8-chloro-2,3-dimethyl quinoline derivatives were designed and synthesized.

Results: The primarily antifungal assay results indicated that all of them exhibited excellent protective efficacy (100%) against Pyricularia oryae at 100 ppm, except compound 2m (90%). Among them, the compound 2p (6-(tert-butyl)-8-chloro-2,3-dimethylquinolin-4-yl(2-chloro-5- (trifluoromethyl)benzyl)carbonate) possessed the highest fungicidal efficacy against Pyricularia oryae, even at 10 ppm.

Conclusion: The structure-activity relationship showed that when the 2-position of benzene ring was substituted by F or Cl, the compound possessed good antifungal activity against Pyricularia oryae.

Keywords: Quinoline, antifungal activity, SAR, benzene, Pyricularia oryae, heterocyclic compounds.

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Article Details

Year: 2018
Page: [1314 - 1318]
Pages: 5
DOI: 10.2174/1570180815666180313121735
Price: $65

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