Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 64, Issue 9, Pages 5603-5619Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.0c02059
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Funding
- National Natural Science Foundation of China [21907019]
- Talent Fund for High-Level University Construction of Guangzhou [B195002009029, B195002009030]
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This study designed and synthesized a series of new membrane-active bakuchiol derivatives, with compound 28 showing potent antibacterial activity against various bacteria and strong in vivo antibacterial efficacy in murine corneal infection models. This design strategy is expected to provide an effective solution to the antibiotic crisis.
Infections caused by drug-resistant bacteria seriously endanger human health and global public health. Therefore, it is urgent to discover and develop novel antimicrobial agents to combat multidrug-resistant bacteria. In this study, we designed and synthesized a series of new membrane-active bakuchiol derivatives by biomimicking the structure and function of cationic antibacterial peptides. The most promising compound 28 displayed potent antibacterial activity against both Gram-positive bacteria (minimum inhibitory concentration, MIC = 1.56-3.125 mu g/mL) and Gram-negative bacteria (MIC = 3.125 mu g/mL), very weak hemolytic activity, and low cytotoxicity. Compound 28 had rapid bactericidal properties and avoided bacterial resistance. More importantly, compound 28 showed strong in vivo antibacterial efficacy against Staphylococcus aureus and Pseudomonas aeruginosa in murine corneal infection models. This design strategy is expected to provide an effective solution to the antibiotic crisis.
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