Antimicrobial evaluation and action mechanism of pyridinium-decorated 1, 4-pentadien-3-one derivatives. Issue 10 (1st June 2018)

• Record Type: Journal Article
• Authors: Zhou, Jian; Tao, Qing-Qing; Wang, Pei-Yi; Shao, Wu-Bin; Wu, Zhi-Bing; Li, Zhong; Yang, Song
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 28:Issue 10(2018)
• Page Start: 1742
• Page End: 1746
• Publication Date: 2018-06-01
• Subjects: Pyridinium -- 1, 4-Pentadien-3-one -- Synthesis -- Action mechanism -- Antimicrobial; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2018.04.034
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: A type of pyridinium-decorated 1, 4-pentadien-3-one derivatives were constructed. Some of the target molecules exerted considerable antimicrobial bioactivities. The minimal EC50 value against Xanthomonas oryzae pv. oryzae is 0.504 µg/mL. A plausible action mechanism for antimicrobial activities was proposed. Abstract: A type of pyridinium-decorated 1, 4-pentadien-3-one derivatives possessing flexible alkyls were designed and synthesized by integrating the key scaffolds of pyridinium cations and 1, 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 µg/mL. A plausible action mechanism for this kind 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.