Synthesis and Evaluation of Colchicine C-Cyclic AmineDerivatives as Potent Anti-Biofilms Agents AgainstMethicillin-Resistant Staphylococcus aureus
Yuxin Yang, Xin Liu, Can Sun, Yuan Fang, Danyang Qu, Zhengbin Tang, Zetao Sun, Xiaoping Zhou, Dacheng Wang
TL;DR
Scientists designed new colchicine derivatives that can inhibit biofilms of MRSA, a dangerous antibiotic-resistant bacteria.
Contribution
New colchicine C-ring amine derivatives were synthesized and shown to inhibit MRSA biofilms and affect key biofilm-related genes.
Findings
Most compounds inhibited MRSA biofilm formation with inhibition rates up to 40.79%.
Compounds 7b–11b showed antibacterial activity or synergistic effects with MICs of 16–32 μg/mL.
The compounds affect biofilm-related genes icaA and agrA, reducing biofilm formation.
Abstract
Background/Objectives: The elimination of bacterial biofilm formation is an effective strategy against bacterial infections. The objective was to design 27 colchicine C-ring modified amine derivatives and evaluate their inhibitory activities against the biofilms of MRSA USA300. Methods: Design 27 colchicine C-ring modified amine derivatives. Evaluate their inhibitory activities against MRSA USA300 biofilms. Conduct antibacterial or synergistic antibacterial experiments. Research the phenotypic mechanisms related to biofilm-related genes icaA and agrA. Results: The experiments showed that most compounds in this series exhibited varying degrees of biofilm inhibitory activity (with inhibition rates ranging from 7.72% to 40.79%). Further verification through antibacterial or synergistic antibacterial experiments revealed that the compounds with biofilm-inhibiting effects (compounds 7b–11b)…
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Taxonomy
TopicsAntimicrobial Peptides and Activities · Peptidase Inhibition and Analysis · Microbial Natural Products and Biosynthesis