In the search for new sources of antimicrobials many researchers have investigated antimicrobial peptides (AMPs) as templates for the design of innovative therapeutics. However, efforts to develop AMPs in this area has been severely hampered by their inherent susceptibility to enzymatic degradation. Given this only a handful of AMPs are currently in clinical trials. Peptide mimetics such as peptoids have emerged as highly promising alternatives to AMPs as they are inherently stable to enzymatic degradation and display potent antimicrobial properties. This feature article highlights the progress that has been made towards the development of novel anti-infective peptoids.
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A study on antimicrobial activity of lysine-like peptoids for the development of new antimicrobials.
Arch Microbiol
January 2025
SLIIT, Malabe, Sri Lanka.
Article Synopsis
- The rise of multidrug-resistant bacteria highlights the urgent need for new antimicrobial medicines, leading to the investigation of antimicrobial peptoids as potential alternatives.
- Thirteen peptoid analogues were synthesized with varying alkyl side chains to analyze their antibacterial properties, and only one, called Tosyl-Octyl-Peptoid (TOP), showed significant broad-spectrum bactericidal activity.
- TOP effectively kills bacteria in both dividing and non-dividing states, demonstrating promising minimum inhibitory concentrations and a high selectivity ratio, suggesting its potential as a future therapeutic option against resistant infections.
Chemical Space for Peptide-based Antimicrobials.
Chimia (Aarau)
October 2024
Department of Chemistry, Biochemistry and Pharmaceutical Sciences, University of Bern, Freiestrasse 3, CH-3012 Bern, Switzerland.
Multidrug-resistant (MDR) bacteria represent a global public health threat, and antimicrobial peptides (AMPs), derived from naturally occurring linear or cyclic peptides, can provide the solution. However, most AMPs are sensitive to proteases and have poor pharmacokinetics. The EU-funded ERC Advanced Grant SPACE4AMPS aims to identify new AMPs by applying the concepts of chemical space and ligand-based virtual screening, which are well known for small molecule drug discovery, to the world of peptides.
View Article and Find Full Text PDFRecent advances in peptoids as promising antimicrobial agents to target diverse microbial species.
Eur J Med Chem
December 2024
Key Laboratory for Green Chemical Process of Ministry of Education, Wuhan Institute of Technology 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, China; Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Wuhan Institute of Technology 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei 430205, China; Hubei Engineering Research Center for Advanced Fine Chemicals, Wuhan Institute of Technology 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, China; School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology 206 1st Rd Optics Valley, East Lake New Technology Development District, Wuhan, Hubei, 430205, China. Electronic address:
The emergence of multidrug-resistant microbial species has become a global health concern, calling for novel antimicrobial agents. Peptoids, a class of synthetic peptidomimetics with unique structural properties, exhibit antimicrobial activity against a broad-spectrum of microbes, in addition to their stability to enzymatic degradation, selectivity, and relative ease of synthesis. Thus, peptoids have great potential in combating various drug-resistant pathogenic microbes.
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Université Clermont Auvergne, Clermont Auvergne INP, CNRS, ICCF, F-63000 Clermont-Ferrand, France.
Bioinspired from cationic antimicrobial peptides, sequence-defined triazolium-grafted peptoid oligomers (6- to 12-mer) were designed to adopt an amphipathic helical polyproline I-type structure. Their evaluation on a panel of bacterial strains (, , , and ), pathogenic fungi (, , and ), and human cells (hRBC, BEAS-2B, Caco-2, HaCaT, and HepG2) enabled the identification of two heptamers with improved activity to selectively fight pathogens. Modulation of parameters such as the nature of the triazolium and hydrophobic/lipophilic side chains, the charge content, and the sequence length drastically potentiates activity and selectivity.
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Department of Pharmaceutical and Cell Biological Chemistry, Pharmaceutical Institute, University of Bonn, 53121, Bonn, Germany. Electronic address:
Dynamics of epigenetic modifications such as acetylation and deacetylation of histone proteins have been shown to be crucial for the life cycle development and survival of Plasmodium falciparum, the deadliest malaria parasite. In this study, we present a novel series of peptoid-based histone deacetylase (HDAC) inhibitors incorporating nitrogen-containing bicyclic heteroaryl residues as a new generation of antiplasmodial peptoid-based HDAC inhibitors. We synthesized the HDAC inhibitors by an efficient multicomponent protocol based on the Ugi four-component reaction.
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