Synthesis and Antibacterial Activities Evaluation of Chalconesemicarbazone Derivatives Bearing 1, 3, 4-Thiadiazole Moiety

被引:0
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作者
Wan Jinlin [1 ]
Wu Shouqun [1 ]
Gan Yiyuan [2 ]
Meng Jiao [2 ]
Wang Zhenchao [2 ]
Ouyang Guiping [2 ]
机构
[1] Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ,Ctr Res Fine Chem, Guiyang 550025, Guizhou, Peoples R China
[2] Guizhou Univ, Coll Pharm, Guiyang 550025, Guizhou, Peoples R China
来源
关键词
1; 3; 4-Thiadiazole; Chalconesemicarbazone; Antibacterial activity; MECHANISM; DESIGN;
D O I
10.7503/cjcu20180081
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A series of chalconesemicarbazone derivatives bearing a 1 ,3 , 4-thiadiazole moiety was designed and synthesized from benzaldehyde and 1 ,3 , 4-thiadiazole. All the target compounds were characterized by means of nuclear magnetic resonance and high resolution mass spectrometer. The preliminary bioassay results indicated that all the title compounds exhibited a certain antibacterial activities in vitro against Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum and Xanthomonas axonopodis pv. citri. Especially, compounds 7j and 7k displayed excellent antibacterial activities (100%) against the above three plant pathogenic bacteria at a concentration of 100 mu g/ mL And the corresponding EC50 (50% effective concentration) values were 15. 13 , 30. 90 , 24. 49 and 21. 33 , 24. 54 , 14. 79 mu g/mL , respectively , which were superior to the commercial antibacterial agent bismerthiazol (92. 23 , 58. 88 and 123. 02 mu g/mL).
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页码:1683 / 1690
页数:8
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