Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 202, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2020.112596
Keywords
Sofalcone; Antimicrobial agents; Drug resistance; Chalcone; Membrane targeting
Categories
Funding
- Talent Fund for High-Level University Construction of Guangzhou [B195002009029, B195002009030]
- National Natural Science Foundation of China
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New antimicrobial agents are urgently needed to overcome drug-resistant bacterial infections. Here we describe the design, synthesis and evaluation of a new class of amphiphilic sofalcone compounds as antimicrobial peptidomimetics. The most promising compound 14, bearing two arginine residues, showed poor hemolytic activity, low cytotoxicity, and excellent antimicrobial activity against Gram-positive bacteria, including MRSA. Compound 14, had good stability in various salt conditions, killed bacteria rapidly by directly disrupting bacterial cell membranes and was slow at developing bacterial resistance. Additionally, compound 14 exhibited effective in vivo efficacy in the murine model of bacterial keratitis caused by Staphylococcus aureus ATCC29213. Our studies suggested that compound 14 possessed promising potential to be used as a novel antimicrobial agent to combat drug-resistant Gram-positive bacteria. (C) 2020 Elsevier Masson SAS. All rights reserved.
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