文献类型：期刊文献

英文题名：Fungicidal activity of novel quinazolin-6-ylcarboxylates and mode of action on Botrytis cinerea

作者：Xu, Jialin[3];Yan, Dongmei[3];Chen, Yongjun[3];Cai, Danni[4];Huang, Fengcheng[3];Zhu, Lisong[3];Zhang, Xianfei[3];Luan, Shaorong[2,4];Xiao, Ciying[5];Huang, Qingchun[1,3]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Chem & Mol Engn, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai, Peoples R China;[4]East China Univ Sci & Technol, Sch Chem & Mol Engn, Shanghai, Peoples R China;[5]East China Univ Sci & Technol, Sch Biochem Engn, Shanghai, Peoples R China

年份：2023

卷号：79

期号：9

起止页码：3022

外文期刊名：PEST MANAGEMENT SCIENCE

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000965456500001)】；

基金：ACKNOWLEDGEMENTS This work was partially supported by the projects of Science and Technology Plan of Shanghai Municipal in China (21S11901400 and 22?N41900100).

语种：英文

外文关键词：quinazolin-6-ylcarboxylates; fungicidal activity; suppressive efficacy; mode of action; Botrytis cinerea

摘要：BACKGROUNDFungal diseases remain important causes of crop failure and economic losses. As the resistance toward current selective fungicides becomes increasingly problematic, it is necessary to develop efficient fungicides with novel chemotypes. RESULTSA series of novel quinazolin-6-ylcarboxylates which combined the structures of pyridine or heterocyclic motif and the N-(3-chloro-4-fluorophenyl)quinazolin-4-amine moiety, a binding group of ATP-binding site of gefitinib, were evaluated for their fungicidal activity on different phytopathogenic fungi. Most of these compounds showed excellent fungicidal activities against Botrytis cinerea and Exserohilum rostratum, especially compound F17 displayed the highest activity with EC50 values as 3.79 mu g mL(-1) against B. cinerea and 2.90 mu g mL(-1) against E. rostratum, which was similar to or even better than those of the commercial fungicides, such as pyraclostrobin (EC50, 3.68, 17.38 mu g mL(-1)) and hymexazol (EC50, 4.56, 2.13 mu g mL(-1)). Moreover, compound F17 significantly arrested the lesion expansion of B. cinerea infection on tomato detached leaves and strongly suppressed grey mold disease on tomato seedlings in greenhouse. The abilities of compound F17 to induce cell apoptosis of the non-germinated spores, to limit oxalic acid production, to reduce malate dehydrogenase (MDH) expression, and to block the active pocket of MDH protein were demonstrated in B. cinerea. CONCLUSIONThe novel quinazolin-6-ylcarboxylates containing ATP-binding site-directed moiety, especially compound F17, could be developed as a potential fungicidal candidate for further study. (c) 2023 Society of Chemical Industry.