Antibacterial Activity of Novel 18β-Glycyrrhetinic Hydrazide or Amide Derivatives  

作　　者：ZHANG Ling FU Yihong DING Yue MENG Jiao WANG Zhenchao WANG Peiyi 

机构地区：[1]State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering,Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Center for R&n of Fine Chemicals,Guizhou University,Guiyang,550025,P.R.China [2]College of Pharmacy,Drug Synthetic Engineering Laboratory of Guizhou Province,Guizhou University,Guiyang,550025,P.R.China

出　　处：《Chemical Research in Chinese Universities》2021年第3期662-667,共6页高等学校化学研究（英文版）

基　　金：This work was supported by the National Natural Science Foundation of China(Nos.21662009,21702037,31860516);the Guizhou Provincial S&T Program,China(Nos.[2017]5788,2018[1051]).

摘　　要：Through a facile structural modification on the natural bioactive ingredient 18β-glycyrrhetinic acid(GA),a series of novel GA hydrazide or amide derivatives was obtained,and their final molecular frameworks were characterized by NMR and HRMS analysis.Antibacterial bioassays revealed that some of the GA hydrazide or amide derivatives were able to suppress the growth of three tested plant pathogens.Particularly,compound 3c exhibited excellent in vitro activity against Xanthomonas oryzae pv.Oryzae(Xoo),Pseudomonas syringae pv.actinidiae(Psa),and Xanthomonas axonopodis pv.citri(Xac),providing the EC_(50) values of 5.89,16.1,and 3.64µg/mL,respectively.The data were better than those of the positive controls thiodiazole copper(92.7,77.8,and 89.9µg/mL,respectively)and bismerthiazol(31.1,125.6,and 77.4µg/mL,respectively).In addition,in vivo experiments suggested that,compared with thiodiazole copper(41.93%and 39.73%,respectively),compound 3c exerted prominently curative and protective activities against rice bacterial leaf blight at 200µg/mL with the control effects of 52.36%and 51.40%,respectively.Given these obtained results,GA hydrazide or amide derivatives could serve as the feasible leads for exploring highly bioactive substrates.

关 键 词：18β-Glycyrrhetinic Hydrazide or amide derivative SYNTHESIS Antibacterial activity 

分 类 号：O62[理学—有机化学]