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Gramicidin-S-Inspired Cyclopeptidomimetics as Potent Membrane-Active Bactericidal Agents with Therapeutic Potential.
- Source :
-
ChemMedChem [ChemMedChem] 2021 Jan 19; Vol. 16 (2), pp. 368-376. Date of Electronic Publication: 2020 Oct 16. - Publication Year :
- 2021
-
Abstract
- Antimicrobial peptides (AMPs) are promising antibacterial agents often hindered by their undesired hemolytic activity. Inspired by gramicidin S (GS), a well-known cyclodecapeptide, we synthesized a panel of antibacterial cyclopeptidomimetics using β,γ-diamino acids (β,γ-DiAAs). We observed that peptidomimetic CP-2 displays a bactericidal activity similar to that of GS while possessing lower side-effects. Moreover, extensive studies revealed that CP-2 likely kills bacteria through membrane disruption. Altogether, CP-2 is a promising membrane-active antibiotic with therapeutic potential.<br /> (© 2020 Wiley-VCH GmbH.)
- Subjects :
- Anti-Bacterial Agents chemical synthesis
Anti-Bacterial Agents chemistry
Dose-Response Relationship, Drug
Gramicidin chemical synthesis
Gramicidin chemistry
Membrane Potentials drug effects
Microbial Sensitivity Tests
Molecular Conformation
Peptidomimetics chemical synthesis
Peptidomimetics chemistry
Structure-Activity Relationship
Anti-Bacterial Agents pharmacology
Bacteria drug effects
Gramicidin pharmacology
Peptidomimetics pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 16
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 33026182
- Full Text :
- https://doi.org/10.1002/cmdc.202000568