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

被引：30

作者：

Fang, Yue-Ming ^{[1
,2
]}

Zhang, Rui-Rui ^{[2
]}

Shen, Zhong-Hua ^{[1
]}

Tan, Cheng-Xia ^{[1
]}

Weng, Jian-Quan ^{[1
]}

Xu, Tian-Ming ^{[2
]}

Liu, Xing-Hai ^{[1
]}

Huang, Hong-Ying ^{[2
]}

Wu, Hong-Ke ^{[1
]}

机构：

[1] Zhejiang Univ Technol, Coll Chem Engn, Hangzhou 310014, Zhejiang, Peoples R China

[2] Zhejiang Base Natl Southern Pesticide Res Ctr, Zhejiang Res Inst Chem Ind, Hangzhou 310023, Zhejiang, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2018年 / 15卷 / 12期

关键词：

Quinoline; antifungal activity; SAR; benzene; Pyricularia oryae; heterocyclic compounds; QUINOLINE DERIVATIVES; THIOUREA; HYBRIDS; FACILE;

D O I：

10.2174/1570180815666180313121735

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1314 / 1318

页数：5

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