Design,synthesis and antifungal activities of novel cis-enamides via intermediate derivatization method  

作　　者：Huiyou Xu Yuyao Sun Hongzuo Li Yunrong Lai Tongchao Zhao Yufei Meng Xiaohong Pan Ran Lin Liyan Song 

机构地区：[1]Key Laboratory of Biopesticide and Chemical Biology,Ministry of Education,College of Plant Protection,Fujian Agriculture and Forestry University,Fuzhou,Fujian,China

出　　处：《Advanced Agrochem》2023年第1期97-103,共7页现代农业化学（英文）

基　　金：financially supported by National Key R&D Program of China(2022 YFD1400700);the Natural Science Foundation of Fujian Province of China(2020J01526);the Foundation of Education Department of Fujian Province of China(JAT21006);the Foundation of Key Laboratory of Biopesticide and Chemical Biology(Keylab2020-03).

摘　　要：On the basis of the structure of natural product lansiumamide B(1),a total of 27 novel cis-enamide compounds were designed and synthesized via Intermediate Derivatization Method.Their chemical structures were characterized by 1H and 13C nuclear magnetic resonance and high-resolution mass spectrometry.The in vitro antifungal activities against Sclerotinia sclerotiorum,Thanatephorus cucumeris and Botrytis cinerea were evaluated by the mycelium linear growth rate method.Most of the compounds showed some activity against each of the fungi at 25 or 50μg/mL.The relationship between structure and antifungal activity was also discussed,which showed the cinnamic double bond was critical to maintain the antifungal activity.Notably,among the title compounds,3e and 3h could inhibit mycelia growth of Botrytis cinerea by approximately 50%(EC_(50))at 39.17 and 41.25μg/mL respectively,which showed better antifungal activity than lansiumamide B(1)with more concise chemical structure.The present study pointed out the correct direction for the development and optimization of lansiumamide B derivatives as potential inhibitors of pathogenic fungi.

关 键 词：Lansiumamide B cis-enamide SYNTHESIS Antifungal Structure activity relationship 

分 类 号：O62[理学—有机化学]