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Synthetic Small Molecules as Anti-biofilm Agents

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 6743

Special Issue Editors


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Guest Editor
University of Palermo Via Archirafi, 90123 Palermo, Italy
Interests: synthesis; heterocycles; antibiotic resistance; drug discovery; antitumor activity

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Guest Editor
Department of Biological Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi, 32-90123 Palermo, Italy
Interests: antibiotic resistance; anti-biofilm agents; anti-virulence compounds; anticancer derivatives; sortase A inhibitors
Special Issues, Collections and Topics in MDPI journals

E-Mail Website
Guest Editor
Department of Biological, Chemical, and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, via Archirafi 32, 90123 Palermo, Italy
Interests: synthesis; reactivity studies of policondensed nitrogen heterocycles; synthesis of marine-derived analogs
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibiotic resistance is a major public health concern, associated with a high social and economic burden. The bacterial ability to form communities, known as biofilms, capable of adhering to abiotic and biotic surfaces is currently considered one of the most important mechanisms of antibiotic resistance, as well as a key virulence factor for many relevant pathogens. Most chronic infections are biofilm-mediated, including pneumonia in cystic fibrosis patients, osteomyelitis, chronic wound infections, and otitis. Additionally, the role of biofilms has recently been recognized both in acute infections and in chronic inflammatory diseases such as Crohn’s disease. Biofilm formation significantly contributes to microbial survival in hostile environments; the bacterial cell was up to 1000 times more resistant within the biofilm with respect to its planktonic form. Contrary to conventional antibiotics, most antibiofilm compounds act as antivirulence agents as they do not affect bacterial growth, imposing a low selective pressure for the onset of antibiotic resistance mechanisms. In the recent decade, many efforts have been made to identify new agents able to interfere with the bacterial biofilm lifecycle, and although many compounds have shown interesting activities for potentially inhibiting biofilm formation or in dispersing preformed biofilms, only a few of these have been validated for their clinical significance using in vivo models. Therefore, much work is still needed in this field.

Prof. Girolamo Cirrincione
Dr. Stella Maria Cascioferro
Dr. Barbara Parrino
Guest Editors

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Keywords

  • antibiofilm compounds
  • antivirulence strategy
  • antibiotic resistance
  • persister cells
  • ESKAPE pathogens

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Published Papers (2 papers)

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Research

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16 pages, 1357 KiB  
Article
Thiazole Analogues of the Marine Alkaloid Nortopsentin as Inhibitors of Bacterial Biofilm Formation
by Anna Carbone, Stella Cascioferro, Barbara Parrino, Daniela Carbone, Camilla Pecoraro, Domenico Schillaci, Maria Grazia Cusimano, Girolamo Cirrincione and Patrizia Diana
Molecules 2021, 26(1), 81; https://doi.org/10.3390/molecules26010081 - 27 Dec 2020
Cited by 37 | Viewed by 2667
Abstract
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections [...] Read more.
Anti-virulence strategy is currently considered a promising approach to overcome the global threat of the antibiotic resistance. Among different bacterial virulence factors, the biofilm formation is recognized as one of the most relevant. Considering the high and growing percentage of multi-drug resistant infections that are biofilm-mediated, new therapeutic agents capable of counteracting the formation of biofilms are urgently required. In this scenario, a new series of 18 thiazole derivatives was efficiently synthesized and evaluated for its ability to inhibit biofilm formation against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923 and S. aureus ATCC 6538 and the Gram-negative strain Pseudomonas aeruginosa ATCC 15442. Most of the new compounds showed a marked selectivity against the Gram-positive strains. Remarkably, five compounds exhibited BIC50 values against S. aureus ATCC 25923 ranging from 1.0 to 9.1 µM. The new compounds, affecting the biofilm formation without any interference on microbial growth, can be considered promising lead compounds for the development of a new class of anti-virulence agents. Full article
(This article belongs to the Special Issue Synthetic Small Molecules as Anti-biofilm Agents)
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Review

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13 pages, 1346 KiB  
Review
Local Oral Delivery Agents with Anti-Biofilm Properties for the Treatment of Periodontitis and Peri-Implantitis. A Narrative Review
by Shorouk Elnagdy, Michail Raptopoulos, Ioannis Kormas, Alessandro Pedercini and Larry F. Wolff
Molecules 2021, 26(18), 5661; https://doi.org/10.3390/molecules26185661 - 17 Sep 2021
Cited by 10 | Viewed by 3337
Abstract
Despite many discoveries over the past 20 years regarding the etiopathogenesis of periodontal and peri-implant diseases, as well as significant advances in our understanding of microbial biofilms, the incidence of these pathologies continues to rise. For this reason, it was clear that other [...] Read more.
Despite many discoveries over the past 20 years regarding the etiopathogenesis of periodontal and peri-implant diseases, as well as significant advances in our understanding of microbial biofilms, the incidence of these pathologies continues to rise. For this reason, it was clear that other strategies were needed to eliminate biofilms. In this review, the literature database was searched for studies on locally delivered synthetic agents that exhibit anti-biofilm properties and their potential use in the treatment of two important oral diseases: periodontitis and peri-implantitis. Full article
(This article belongs to the Special Issue Synthetic Small Molecules as Anti-biofilm Agents)
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