The synthesis of 6-(tert-butyl)-8-fluoro-2,3-dimethylquinoline carbonate derivatives and their antifungal activity against Pyricularia oryzae

2019, Volume 13, Issue 2

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Frontiers of Chemical Science and Engineering >> 2019, Volume 13, Issue 2 doi: 10.1007/s11705-018-1734-7

The synthesis of 6-(tert-butyl)-8-fluoro-2,3-dimethylquinoline carbonate derivatives and their antifungal activity against Pyricularia oryzae

. College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.. Zhejiang Base of National Southern Pesticide Research Centre, Zhejiang Research Institute of Chemical Industry, Hangzhou 310023, China

Accepted: 2018-07-17 Available online: 2018-07-17

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Abstract

A series of novel 6-( -butyl)-8-fluoro-2,3-dimethylquinoline carbonate derivatives were designed and synthesized. Bioassay results showed that some of them exhibited good activity against ( ). It was found that the compound (benzyl (6-( -butyl)-8-fluoro-2,3- dimethylquinolin-4-yl) carbonate) possessed good activity against whatever protective activity (10 mg·L ) or curative activity (25 mg·L ), which was better than that of control tebufloquin. In addition, the frontier molecular orbit results revealed that the compound held higher activity against when the total energy was low and the ClogP was high, which may provide useful information for further design novel fungicides.

Keywords

quinoline ; synthesis ; antifungal activity ; rice blast ; SAR

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