Issue 34, 2022

Discovery of antibacterial agents targeting biofilm formation: total synthesis and in vitro investigation of amycolasporins

Abstract

Three monoterpene alkaloids amycolasporin A and (±) amycolasporins B and C have been synthesized for the first time from commercially available materials in yields of 31%, 14% and 21%, respectively. Their six analogues (18, 19, 30a and 30d–30f) were synthesized through a similar protocol. Meanwhile, the antibacterial activity of all synthesized molecules was evaluated, showing different levels of bioactivity. Among them, analogue 30d was screened as the most effective antibacterial candidate against E. coli (MIC value, 12.5 μg mL−1) and S. aureus (MIC value, 12.5 μg mL−1). Further investigation showed that 30d obviously inhibited biofilm formation and disrupted the preformed biofilm of E. coli and S. aureus by promoting intracellular ROS release.

Graphical abstract: Discovery of antibacterial agents targeting biofilm formation: total synthesis and in vitro investigation of amycolasporins

Supplementary files

Article information

Article type
Paper
Submitted
28 Jun 2022
Accepted
05 Aug 2022
First published
08 Aug 2022

Org. Biomol. Chem., 2022,20, 6831-6843

Discovery of antibacterial agents targeting biofilm formation: total synthesis and in vitro investigation of amycolasporins

W. Wu, Y. Mu, J. Tan, Z. Wang, C. Zhang, G. Li, Y. Jin, X. Huang and L. Han, Org. Biomol. Chem., 2022, 20, 6831 DOI: 10.1039/D2OB01166B

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