Abstract:
:Antimicrobial peptides (AMPs) are amphipathic molecules displaying broad-spectrum bactericidal activity, providing opportunities to develop a new generation of antibiotics. However, their use is limited either by poor metabolic stability or by high hemolytic activity. We herein addressed the potential of thiazole-based γ-peptide oligomers named ATCs as tunable scaffolds to design polycationic AMP 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_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Bonnel C,Legrand B,Simon M,Clavié M,Masnou A,Jumas-Bilak E,Kang YK,Licznar-Fajardo P,Maillard LT,Masurier Ndoi
10.1021/acs.jmedchem.0c00077subject
Has Abstractpub_date
2020-09-10 00:00:00pages
9168-9180issue
17eissn
0022-2623issn
1520-4804journal_volume
63pub_type
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