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Special Issue "Drug Targeting towards Fighting Pathogen Bacteria"

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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (31 May 2023) | Viewed by 5436

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Dr. Sandra N. Pinto

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Institute for Bioengineering and Biosciences and i4HB—Institute for Health and Bioeconomy, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal
Interests: nanomaterials; antimicrobial polymers; antimicrobial peptides; anticancer polymers; bacterial biofilms; biophysics; confocal and two-photon microscopy

Special Issue Information

Dear Colleagues,

One of the major public health concerns of the 21st century is the continuous emergence of antibiotic-resistant strains, which cause a serious threat to the efficient prevention and treatment of bacterial-related infections.

Antibiotic resistance can be considered an inevitable consequence of the rambunctious and unregulated use of antibiotics, which remains a major factor facilitating the emergence of antibiotics resistance worldwide.

Several fields of medicine depend on the availability of antibiotic drugs; for instance, the immunosuppression induced by cancer therapy and long-term vascular catheter placement make cancer patients susceptible to bacterial infections often caused by resistant organisms, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Thus, to avoid secondary infections, cancer patients are routinely given antibiotics, which cause many side effects, including antimicrobial resistance.

Conventional antibiotics have many disadvantages, such as the development of resistance and, in some cases, a low therapeutic index. Thus, more efficient and effective compounds are urgently required.

This Special Issue aims to identify novel strategies and/or compounds that can help improve the success of bacterial treatment.

In this Special Issue, original research articles and reviews are welcome. Research areas may include (but are not limited to) the following:

Antimicrobial polymers;
Antimicrobial peptides and peptidomimetics;
Use of natural products;
Combinations of antimicrobial agents effect;
Inhibitors of virulence factors;
Use of nanoparticles;
Drug delivery systems;
Topical antimicrobial treatment;
Phage therapy;
Enzybiotics.

This Special Issue welcomes different types of submissions, such as original research papers, short communications, reviews, case reports, and opinion papers.

I look forward to receiving your contributions.

Dr. Sandra N. Pinto
Guest Editor

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Keywords

antimicrobial compounds
antibiotic resistance
antibiotics
bacterial infections
antimicrobial strategies

Published Papers (4 papers)

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Research

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Open AccessArticle

Targeting Siderophore-Mediated Iron Uptake in M. abscessus: A New Strategy to Limit the Virulence of Non-Tuberculous Mycobacteria

Giuseppe F. Mangiatordi

and

Pharmaceutics 2023, 15(2), 502; https://doi.org/10.3390/pharmaceutics15020502 - 02 Feb 2023

Cited by 1 | Viewed by 879

Abstract

Targeting pathogenic mechanisms, rather than essential processes, represents a very attractive approach for the development of new antimycobacterial drugs. In this context, iron acquisition routes have recently emerged as potentially druggable pathways. However, the importance of siderophore biosynthesis in the virulence and pathogenicity of M. abscessus (Mab) is still poorly understood. In this study, we investigated the Salicylate Synthase (SaS) of Mab as an innovative molecular target for the development of inhibitors of siderophore production. Notably, Mab-SaS does not have any counterpart in human cells, making it an interesting candidate for drug discovery. Starting from the analysis of the binding of a series of furan-based derivatives, previously identified by our group as inhibitors of MbtI from M. tuberculosis (Mtb), we successfully selected the lead compound 1, exhibiting a strong activity against Mab-SaS (IC₅₀ ≈ 5 µM). Computational studies characterized the key interactions between 1 and the enzyme, highlighting the important roles of Y387, G421, and K207, the latter being one of the residues involved in the first step of the catalytic reaction. These results support the hypothesis that 5-phenylfuran-2-carboxylic acids are also a promising class of Mab-SaS inhibitors, paving the way for the optimization and rational design of more potent derivatives. Full article

(This article belongs to the Special Issue Drug Targeting towards Fighting Pathogen Bacteria)

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Open AccessArticle

Exploring the Antimicrobial and Pharmacological Potential of NF22 as a Potent Inhibitor of E. coli DNA Gyrase: An In Vitro and In Silico Study

and

Pharmaceutics 2022, 14(12), 2768; https://doi.org/10.3390/pharmaceutics14122768 - 10 Dec 2022

Viewed by 789

Abstract

Toward the search for novel antimicrobial agents to control pathogenic E. coli-associated infections, a series of novel norfloxacin derivatives were screened for antimicrobial activities. The norfloxacin derivative, 1-ethyl-6-fluoro-7-(4-(2-(2-(3-hydroxybenzylidene)hydrazinyl)-2-oxoethyl)piperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (NF22) demonstrated excellent antibacterial activities against E. coli ATCC 25922 (MIC = 0.0625 μg/mL) and MDR E. coli 1–3 (MIC = 1, 2 and 1 µg/mL). The time-kill kinetic studies have demonstrated that the NF22 was advantageous over norfloxacin and ciprofloxacin in killing the control and MDR E. coli strains. The checkerboard assay showed that NF22 in combination with tetracycline had a synergistic effect against the E. coli strains. The experimental findings are supported by molecular modeling studies on DNA gyrase, explaining the interactions involved for compound NF22, compared to norfloxacin and ciprofloxacin. Further, the compound was also evaluated for various pharmacokinetics (absorption, metabolism, distribution, toxicity and excretion) as well as drug-likeness properties. Our data have highlighted the potential of norfloxacin by restoring its efficacy against E. coli which could lead to the development of new antimicrobial agents. Full article

(This article belongs to the Special Issue Drug Targeting towards Fighting Pathogen Bacteria)

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Open AccessArticle

Cecropin A Improves the Antibacterial Activity of Hen Egg White Lysozyme against Challenging Salmonella enterica Serovars

and

Pharmaceutics 2022, 14(10), 2201; https://doi.org/10.3390/pharmaceutics14102201 - 16 Oct 2022

Viewed by 947

Abstract

The prevalence of multidrug-resistant Salmonella enterica among animal- and plant-derived food products threatens global healthcare and economic sectors. Hen egg white lysozyme is widely exploited as a food preservative against Gram-positive pathogens. Nevertheless, its limited penetration of the outer membrane renders it ineffective against Gram-negative bacteria. Herein, we present a safe and effective approach to facilitate HEWL access to peptidoglycan layers using cecropin A. In silico analysis of cecropin A peptide revealed an amphipathic α-helical peptide with potential outer membrane permeabilizing activity through its interaction with both hydrophobic and ionic stabilizing forces. Evaluation of HEWL/cecropin A combination showed a cecropin A dose-dependent bacterial count reduction up to 4.16 and 3.18 ± 0.26 log units against Salmonella enterica ATCC 35664 at the logarithmic and stationary growth phases, respectively. Moreover, the combination displayed antibacterial activity of 2.1 ± 0.31 and ~1 log-unit reductions against Salmonella enterica serovars Kentucky, Typhimurium, and Enteritidis, respectively, whereas Hato and Shangani were found irresponsive. The cytotoxicity assay revealed compatibility of cecropin A with oral epithelial cells. These observations suggest HEWL/cecropin A combination as an effective and safe alternative to lysozyme against Salmonella enterica. Full article

(This article belongs to the Special Issue Drug Targeting towards Fighting Pathogen Bacteria)

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Review

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Open AccessReview

Fluoroquinolones Hybrid Molecules as Promising Antibacterial Agents in the Fight against Antibacterial Resistance

Ioana-Andreea Lungu

Octavia-Laura Moldovan

Victoria Biriș

and

Aura Rusu

Pharmaceutics 2022, 14(8), 1749; https://doi.org/10.3390/pharmaceutics14081749 - 22 Aug 2022

Cited by 9 | Viewed by 2323

Abstract

The emergence of bacterial resistance has motivated researchers to discover new antibacterial agents. Nowadays, fluoroquinolones keep their status as one of the essential classes of antibacterial agents. The new generations of fluoroquinolones are valuable therapeutic tools with a spectrum of activity, including Gram-positive, Gram-negative, and atypical bacteria. This review article surveys the design of fluoroquinolone hybrids with other antibacterial agents or active compounds and underlines the new hybrids’ antibacterial properties. Antibiotic fluoroquinolone hybrids have several advantages over combined antibiotic therapy. Thus, some challenges related to joining two different molecules are under study. Structurally, the obtained hybrids may contain a cleavable or non-cleavable linker, an essential element for their pharmacokinetic properties and mechanism of action. The design of hybrids seems to provide promising antibacterial agents helpful in the fight against more virulent and resistant strains. These hybrid structures have proven superior antibacterial activity and less susceptibility to bacterial resistance than the component molecules. In addition, fluoroquinolone hybrids have demonstrated other biological effects such as anti-HIV, antifungal, antiplasmodic/antimalarial, and antitumor activity. Many fluoroquinolone hybrids are in various phases of clinical trials, raising hopes that new antibacterial agents will be approved shortly. Full article

(This article belongs to the Special Issue Drug Targeting towards Fighting Pathogen Bacteria)

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