Li, Na; Liu, Dan; Dai, Jiang-Kun; Wang, Jin-Yi; Wang, Jun-Ru published the artcile< Synthesis and in vitro antibacterial activity of quaternized 10-methoxycanthin-6-one derivatives>, Category: chlorides-buliding-blocks, the main research area is benzyl methoxycanthinone preparation agrochem antibacterial activity SAR; 10-methoxycanthin-6-one; SARs; antibacterial; quaternization.
Background: Based on our previous work, we found that 10-methoxycanthin-6-one displayed potential antibacterial activity and quaternization was an available method for increasing the antibacterial activity. Here, we explored the antibacterial activity of quaternized 10-methoxy canthin-6-one derivatives Methods and Results: Twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by the double dilution method. Moreover, the structure-activity relationships (SARs) were carefully summarized in order to guide the development of antibacterial canthin-6-one agents. Two highly active compounds displayed 8-fold superiority (MIC = 3.91 μg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae compared to agrochem. streptomycin sulfate, and showed potential activity against B. cereus. Moreover, these two compounds exhibited good “”drug-like”” properties, low cytotoxicity, and no inhibition on seed germination. Conclusions: This work provides two new effective quaternized canthin-6-one derivatives as candidate bactericide, promoting the development of natural-sourced bactericides and preservatives.
Molecules published new progress about Agrochemical antibacterial agents. 611-19-8 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H6Cl2, Category: chlorides-buliding-blocks.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics