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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• 作者：Pei Li ; Li Shi ; Xia Yang ; Lei Yang ; Xue-Wen Chen ; Fang Wu ; Qing-Cai Shi ; Wei-Ming Xu ; Ming He ; De-Yu Hu ; Bao-An Song ; ^{songbaoan22@yahoo.com" class="auth_mail}
• 关键词：Xoo ; Xanthomonas oryzae pv. oryzae ; Xoc ; Xanthomonas oryzae pv. oryzicolaby ; EC50 ; half-maximal effective concentration ; 1H NMR ; 1H nuclear magnetic resonance ; 13C NMR ; 13C nuclear magnetic resonance ; IR ; infrared spectroscopy ; SAR ; structure&ndash ; activity relationship
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 April, 2014
• 年：2014
• 卷：24
• 期：7
• 页码：1677-1680
• 全文大小：470 K

文摘

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 渭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%).