Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 186, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.111901
Keywords
AA peptides; Peptidomimetics; Antimicrobial; Bacterial resistance; Solid-phase synthesis
Categories
Funding
- NSF [1708500]
- NIH [1R01GM112652]
- Direct For Mathematical & Physical Scien
- Division Of Materials Research [1708500] Funding Source: National Science Foundation
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Development of novel antimicrobial agents combating drug resistance is in an urgent need. Herein we report the design and synthesis of a series of short lipo-alpha/sulfono-gamma-AA hybrid peptides. Several short peptides exhibit potent and broad-spectrum antimicrobial activity toward both Gram-positive and Gram-negative bacteria. Membrane depolarization and fluorescence microscopy studies indicate that these short lipo-alpha/sulfono-gamma-AA hybrid peptides can mimic the mechanisms of HDPs to kill bacteria by disrupting bacterial membranes. In addition, these short peptides also show capability to eradicate the biofilm formation of E. coli even at very low concentration. The further development of lipidated alpha/sulofono-gamma-AA hybrid peptides may lead to a new class of antibiotic agents to combat drug resistance. (C) 2019 Elsevier Masson SAS. All rights reserved.
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