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Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity providing opportunities to develop new generation of antibiotics. However their use is limited either by poor metabolic stability or high… Click to show full abstract
Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity providing opportunities to develop new generation of antibiotics. However their use is limited either by poor metabolic stability or high hemolytic activity. We herein addressed the potential of thiazole-based γ-peptide oligomers named ATCs as tunable scaffolds to design poly-cationic AMPs mimetics. Knowing the side chain distribution along the backbone, we rationally designed facially amphiphilic sequences with bactericidal effect in the micromolar range. Since no hemolytic activity was detected up to 100 µM, this class of compounds has shown the potential for therapeutic development.
Journal Title: Journal of medicinal chemistry
Year Published: 2020
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