Li Pei, Shi Li, Gao Man-Ni, Yang Xia, Xue Wei, Jin Lin-Hong, Hu De-Yu, Song Bao-An
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, PR China.
Bioorg Med Chem Lett. 2015 Feb 1;25(3):481-4. doi: 10.1016/j.bmcl.2014.12.038. Epub 2014 Dec 19.
In this study, a series of 2-mercapto-5-substituted-1,3,4-oxadiazole/thiadiazole derivatives were synthesized and evaluated for their antibacterial activities against rice bacterial leaf blight and tomato bacterial wilt caused by Xanthomonas oryzae pv. oryzae (Xoo) and Ralstonia solanacearum (R. solanacearum) via the turbidimeter test in vitro. Antibacterial bioassays indicated that most compounds demonstrated appreciable antibacterial bioactivities against Xoo and R. solanacearum. Among the title compounds, compound 4i demonstrated the best inhibitory effect against Xoo and R. solanacearum with half-maximal effective concentration (EC50) values of 14.69 and 15.14μg/mL, respectively, which were even better than those of commercial agents Bismerthiazol and Thiodiazole Copper. In vivo antibacterial activities tests under greenhouse conditions revealed that the control efficiency of compound 4i against rice bacterial leaf blight and tobacco bacterial wilt were better than those of Bismerthiazol and Thiodiazole Copper. Meanwhile, field trials also indicated that compound 4i demonstrated appreciable control efficiency against rice bacterial leaf blight and tomato bacterial wilt.
在本研究中,合成了一系列2-巯基-5-取代-1,3,4-恶二唑/噻二唑衍生物,并通过体外比浊法测试评估了它们对由水稻白叶枯病菌(Xanthomonas oryzae pv. oryzae,Xoo)和青枯雷尔氏菌(Ralstonia solanacearum,R. solanacearum)引起的水稻白叶枯病和番茄青枯病的抗菌活性。抗菌生物测定表明,大多数化合物对Xoo和R. solanacearum表现出明显的抗菌生物活性。在标题化合物中,化合物4i对Xoo和R. solanacearum表现出最佳抑制效果,其半数有效浓度(EC50)值分别为14.69和15.14μg/mL,甚至优于商业药剂叶枯唑和噻菌铜。温室条件下的体内抗菌活性测试表明,化合物4i对水稻白叶枯病和烟草青枯病的防治效果优于叶枯唑和噻菌铜。同时,田间试验也表明,化合物4i对水稻白叶枯病和番茄青枯病表现出明显的防治效果。