期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 28, 期 10, 页码 1742-1746出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.04.034
关键词
Pyridinium; 1,4-Pentadien-3-one; Synthesis; Action mechanism; Antimicrobial
资金
- Key Technologies RD Program [2014BAD23B01]
- National Natural Science Foundation of China [21372052, 21662009]
- Ministry of Education of China [20135201110005, 213033A]
- Guizhou Provincial ST Program [[2012]6012, [2016]1029]
A type of pyridinium-decorated l,4-pentadien-3-one derivatives possessing flexible alkyls were designed and synthesized by integrating the key scaffolds of pyridinium cations and l,4-pentadien-3-one skeleton in a single molecular architecture. Antimicrobial bioassays indicated that some of the target molecules exerted considerable bioactivities against six phytopathogenic strains, especially for Xanthomonas oryzae pv. oryzae, the minimal EC50 value can reach to 0.504 mu g/mL. A plausible action mechanism for this land of compounds was proposed and confirmed by employing fluorescent spectroscopy, fluorescence microscopy, and scanning electron microscopy. We anticipated that this finding can promote high-efficient lead compounds discovery in the research of antimicrobial chemotherapy. (C) 2018 Elsevier Ltd. All rights reserved.
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