The discovery of new scaffold of plant activators:From salicylic acid to benzotriazole  

The discovery of new scaffold of plant activators:From salicylic acid to benzotriazole

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作  者:Kang Chang Jian-Qin Chen Yan-Xia Shi Mei-Jian Sun Peng-Fei Li Zhen-Jiang Zhao Wei-Ping Zhu Hong-Lin Li Yu-Fang Xu Bao-Ju Li Xu-Hong Qian 

机构地区:[1]State Key Laboratory of Bioreactor Engineering, 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, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China [3]Institute of Vegetables and Flowers, Chinese Academy of AgricuRural Science, Beijing 100081, China

出  处:《Chinese Chemical Letters》2017年第4期919-926,共8页中国化学快报(英文版)

基  金:financially supported by the National Basic Research Program of China(973 Program,No.2010CB126100);the National High Technology Research and Development Program of China(863 Program,No.2011AA10A207);the Shanghai Leading Academic Discipline Project(B507);the Fundamental Research Funds for the Central Universities

摘  要:Started from salicylic acid(SA) and related commercialized plant activators,based on molecular threedimensional shape and pharmacophore similarity comparison(SHAFTS),a new lead compound benzotriazole was predicted and a series of benzotriazole derivatives were designed and synthesized.The bioassay showed that benzotriazole had high activity against a broad spectrum of diseases including fungi and oomycetes in vivo,but no activity in vitro.And the introduction of proper groups at the1'-position and 5'-position was beneficial to the activity.So,they had the potential to be exploited as novel plant activators.Started from salicylic acid(SA) and related commercialized plant activators,based on molecular threedimensional shape and pharmacophore similarity comparison(SHAFTS),a new lead compound benzotriazole was predicted and a series of benzotriazole derivatives were designed and synthesized.The bioassay showed that benzotriazole had high activity against a broad spectrum of diseases including fungi and oomycetes in vivo,but no activity in vitro.And the introduction of proper groups at the1'-position and 5'-position was beneficial to the activity.So,they had the potential to be exploited as novel plant activators.

关 键 词:Plant activator Systemic acquired resistance Salicylic acid Benzotriazole Virtual screening 

分 类 号:TQ459[化学工程—农药化工]

 

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