Design, synthesis, and antibacterial activity against rice bacterial leaf blight and leaf streak of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivative
Design, synthesis, and antibacterial activity against rice bacterial leaf blight and leaf streak of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivative
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DOI：
10.1016/j.bmcl.2014.02.060
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发表时间：
2014-04-01
影响因子：
2.7
通讯作者：
Song, Bao-An
中科院分区：
文献类型：
--
作者：
Li, Pei;Shi, Li;Song, Bao-An
合成了一系列2，5-取代-1，3，4-恶二唑/噻二唑砜衍生物，并对其对水稻白叶枯病和条斑病的抑菌活性进行了评价。水稻白叶枯病菌（Xanthomonas oryzae pv.）通过体外浊度法测定。抑菌活性测试结果表明，大部分化合物对水稻白叶枯病和条斑病具有较好的抑制作用。其中化合物6c对水稻白叶枯病和条斑病的抑制效果最好，其半最大有效浓度（EC_（50））分别为1.07和7.14 μ g/mL，优于市售的噻二唑和噻二唑铜。室内抑菌活性试验表明，化合物6c和6 g对水稻白叶枯病的防治效果分别为43.5%和42.4%，优于噻菌唑和噻二唑铜的防治效果（分别为25.5%和37.5%）。(C)2014爱思唯尔有限公司版权所有。
A series of 2,5-substituted-1,3,4-oxadiazole/thiadiazole sulfone derivatives were synthesized and evaluated for their antibacterial activities against rice bacterial leaf blight and leaf streak caused by Xanthomonas oryzae pv. oryzae and Xanthomonas oryzae pv. oryzicolaby via the turbidimeter test in vitro. Antibacterial bioassay results indicated that most compounds demonstrated good inhibitory effect antibacterial bioactivities against rice bacterial leaf blight and leaf streak. Among the title compounds, compound 6c demonstrated the best inhibitory effect against rice bacterial leaf blight and leaf streak with half-maximal effective concentration (EC50)values of 1.07 and 7.14 mu g/mL, respectively, which were even better than those of commercial agents such as Bismerthiazol and Thiediazole Copper. In vivo antibacterial activities tests at greenhouse conditions demonstrated that the controlling effect of compounds 6c (43.5%) and 6g (42.4%) against rice bacterial leaf blight were better than those of Bismerthiazol (25.5%) and Thiediazole Copper (37.5%). (C) 2014 Elsevier Ltd. All rights reserved.