ChemMedChem
ChemMedChem
5 years ago

Potent Antimicrobial Activity of Lipidated Short α,γ-Hybrid Peptides

Potent Antimicrobial Activity of Lipidated Short α,γ-Hybrid Peptides
Sushil N. Benke, Hosahudya N. Gopi, Hirekodathakallu V. Thulasiram
Herein we report the potent antimicrobial activity of α,γ-hybrid lipopeptides composed of 1:1 alternating α- and γ-amino acids. Along with their potent antimicrobial activity against various Gram-positive and Gram-negative bacteria, these hybrid lipopeptides were found to be less hemolytic. Studies into the mechanism of action revealed that these short cationic lipopeptides bind and disrupt the bacterial cell membrane. Time–kill kinetics analyses revealed that the potent α,γ-hybrid lipopeptides completely inhibit bacterial growth in less than 20 minutes. Overall, the promising antimicrobial activity along with lower hemolytic activity displayed by these α,γ-hybrid lipopeptides make them well suited for further exploration into the design of potent lipopeptide antibiotics. The disruptors: Herein we report the design, synthesis, and potent antimicrobial activity of short α,γ-hybrid lipopeptides composed of 1:1 alternating α- and γ-amino acids. Investigation of the mechanism of action revealed that these short cationic lipopeptides bind and disrupt the bacterial cell membrane.

Publisher URL: http://onlinelibrary.wiley.com/resolve/doi

DOI: 10.1002/cmdc.201700370

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