Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 18, Pages 4294-4297Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.08.040
Keywords
Pyridinium; Carbazole; Synthesis; Optimization; Antibacterial
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Funding
- Key Technologies RD Program [2014BAD23B01]
- National Natural Science Foundation of China [21372052, 21662009]
- Ministry of Education of China [NCET-13-0748, 213033A]
- Guizhou Provincial ST Program [[2012]6012, [2016]1029, 201341]
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Various pyridinium-functionalized carbazole derivatives were constructed by coupling the key fragments of carbazole skeleton and pyridinium nucleus in a single molecular architecture. Antibacterial bioassays revealed that some of the title compounds displayed impressive bioactivities against plant pathogens such as Xanthomonas oryzae pv. oryzae, Ralstonia solanacearum, and Xanthomonas axonopodis pv. citri with minimal EC50 values of up to 0.4, 0.3, and 0.3 mg/L, respectively. These bioactivities were achieved by systematically tuning and optimizing bridging linker, alkyl length of the tailor, and substituents on the carbazole scaffold. Compared with the bioactivity of the lead compound (AP-10), antibacterial efficacy dramatically increased by approximately 13-, 104- and 21-fold. This finding suggested that these compounds can serve as new lead compounds in research on antibacterial chemotherapy. (C) 2017 Elsevier Ltd. All rights reserved.
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