Antimicrobial Agents: Synthesis and Design
A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Microbiology".
Deadline for manuscript submissions: closed (20 September 2025) | Viewed by 1099
Special Issue Editor
Interests: nanomaterials; dendrimers; macromolecules; hydrogels for biomedical and environmental applications; resins; polymeric drug delivery systems; organic synthesis; antibacterial and/or antitumor cationic macromolecules; solubilizing agents; cationic bola-amphiphiles
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Special Issue Information
Dear Colleagues,
Multidrug-resistant (MDR) pathogens, often responsible for severe and incurable infections, are a worldwide concern urgently requiring efforts to find new treatment options. Both Gram-negative and Gram-positive MDR bacilli are emerging as clinically relevant superbugs, especially those included in the ESKAPE family, comprehending Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterococci. From years, several of such bacteria have demonstrated a promising sensitivity against natural cationic antimicrobial peptides (AMPs) acting by an extra-genomic mechanism with a low tendency to develop resistance, mainly based on cytoplasmic membrane disruption. On this evidence, more stable and low-cost cationic molecules and macromolecules, mimicking AMPs, are continuously synthesized and tested on various pathogenic bacterial species. Synthetic phosphonium bola-amphiphiles (BAs) molecules bearing two cationic triphenyl phosphonium groups, linked by a C12 hydrophobic chain, have recently revealed potent sterilizing effects against a series of environmental bacteria and very potent antibacterial effects against 50 clinical isolates of both Gram-positive and Gram-negative species with a difficult pattern of resistance, thus disabling the current viable to functioning. These recent achievements open a new area still largely unexplored, concerning the possible use of new antibacterial compounds, achievable by merging the properties of the known quaternary phosphonium and ammonium salts with the colloidal ones of BAs, which enable them to self-assemble nanomicelles in water. In a worrying scenario showing the incessant decline in the number of effective antibiotics and the rising healthcare costs due to increasingly frequent hospitalizations, this Special Issue aims to include articles and reviews on cationic natural and synthetic molecules and macromolecules, including BA and structural strategies to improve their antibacterial activity, selectivity, and carrying capacity, as well as studies investigating molecular mechanisms of action. Furthermore, studies of formulations of the developed agents, characterized by antibacterial activity and low cytotoxicity toward mammalian cells, will be welcome.
Prof. Dr. Silvana Alfei
Guest Editor
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Keywords
- multi-drug resistant Gram-negative and Gram-positive pathogens
- clinically relevant superbugs
- severe and almost untreatable infections
- immunocompromised individuals
- synthetic antimicrobial cationic macromolecules
- synthetic cationic dendrimers, polymers, and copolymers
- polymerizing strategies
- quaternary ammonium and phosphonium salts
- amino-acid modified macromolecules
- electrostatic interactions and membrane permeabilization
- membrane disruptors
- drug delivery systems
- cationic bola-amphiphiles
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