Design,synthesis and bioassay of the emerging photo-responsive fungicides  

作　　者：Wen Fu Xinyue Hu Qinglong Yuan Zhiping Xu Jiagao Cheng Zhong Li Xusheng Shao 

机构地区：[1]Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [2]State Key Laboratory of Bioreactor Engineering,East China University of Science and Technology,Shanghai 200237,China [3]Shanghai Frontier Science Research Base of Optogenetic Techniques for Cell Metabolism,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [4]Engineering Research Center of Pharmaceutical Process Chemistry,Ministry of Education,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China

出　　处：《Chinese Chemical Letters》2023年第8期223-226,共4页中国化学快报（英文版）

基　　金：This work was financially supported by the Natural Science Foundation of China(Nos.21877039,32072441);National Key Research and Development Program of China(No.2018YFD0200100);Innovation Program of Shanghai Municipal Education Commission(No.2017-01-07-00-02-E00037).

摘　　要：Precise and spatiotemporal control over the pesticide remains to be a challenge.More efficient controlled release systems(CRSs)have been developed to support the precise delivery of active ingredients.Herein,we incorporated the photoremovable protecting groups(PRPGs)into phenamacril(PHE)and obtained two photo-responsive fungicides of NV-PHE and DEACM-PHE.The 4,5-dimethoxy-o-nitrobenzyl(NV)or 7-diethylaminocoumarin(DEACM)-caged PHE could release the active molecule PHE after irradiation of UV light and blue light,respectively.Optical properties and in-vitro/vivo fungicidal activities of NV-PHE and DEACM-PHE demonstrated the feasibility for light controlled release of PHE.DEACM-PHE could release 98%PHE by illumination of blue light.The irradiated DEACM-PHE could preserve the similar bioactivity of PHE,and significantly improve the in-vitro/vivo fungicidal activities compared to the non-irradiated DEACM-PHE.The optical controlled release of PHE from DEACM-PHE enabled the precise and spatiotemporal delivery of PHE,diversifying the development of CRSs for pesticide,and providing environmentfriendly agricultural applications with high pesticide efficiency.

关 键 词：Phenamacril Controlled release Photoremovable protecting groups SPATIOTEMPORAL Significant difference 

分 类 号：TQ455.4[化学工程—农药化工]