期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 4, 页码 1214-1217出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.01.029
关键词
1,3,4-Oxadiazole; Pyridinium; Amphiphile; Synthesis; Antibacterial
资金
- National Natural Science Foundation of China - China [21372052, 21202025]
- Key Technologies RD Program [2014BAD23B01]
- Research Project of Chinese Ministry of Education [213033A, 20135201110005]
- Guizhou Province ST Program [[2012] 6012, [2011] 3016]
- Scientific Research Foundation for the Introduced Talents of Guizhou University [[2015]34]
By introducing the pyridinium group into 2,5-substituted-1,3,4-oxadiazole, a series of pyridinium-tailored 2,5-substituted-1,3,4-oxadiazole thioether/sulfoxide/sulfone derivatives were obtained, and their antibacterial activities were evaluated via turbidimeter test in vitro. The bioassays reveal that most of the target compounds exhibit better inhibition activities against pathogen Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri than positive controls bismerthiazol (CK1) or thiodiazole copper (CK2). Among them, I-8, I-10, I-12, II-10, II-12, III-10, and III-12 exert excellent inhibition activities against the three pathogenic bacteria with the half-maximal effective concentration (EC50) values ranging from 0.54 to 12.14 mu g/mL. Our results demonstrate that pyridinium-tailored 1,3,4-oxadiazole thioether/sulfoxide/sulfone derivatives can serve as potential alternative bactericides for the management of plant bacterial diseases. (C) 2016 Elsevier Ltd. All rights reserved.
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