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

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

Volume: 15 Issue: 12

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 and Hong-Ke Wu

Affiliation:

• Zhejiang Base of National Southern Pesticide Research Centre, Zhejiang Research Institute of Chemical Industry, Hangzhou 310023,China

• College of Chemical Engineering, Zhejiang University of Technology, Hangzhou, 310014,China

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

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.

Cite this article as:

Fang Yue-Ming, Zhang Rui-Rui , Shen Zhong-Hua, Tan Cheng-Xia, Weng Jian-Quan, Xu Tian-Ming *, Liu Xing-Hai*, Huang Hong-Ying and Wu Hong-Ke, Synthesis and Antifungal Activity of Some 6-tert-butyl-8-chloro-2, 3-dimethylquinolin-4-ol Derivatives against Pyricularia oryae, Letters in Drug Design & Discovery 2018; 15 (12) . https://dx.doi.org/10.2174/1570180815666180313121735