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Antibiotics
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Antibacterial Drug Discovery
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Antibacterial Drug Discovery

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Antibiotics Use and Antimicrobial Stewardship".

Deadline for manuscript submissions: closed (31 December 2020) | Viewed by 21051

Special Issue Editor

Dr. Björn Windshügel

E-Mail Website
Guest Editor
Fraunhofer Institute for Molecular Biology and Applied Ecology IME, ScreeningPort, Hamburg, Germany
Interests: efflux pumps; antibiotic adjuvants; structure-based drug design
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The emergence of multidrug resistant and extensively drug resistant bacteria, in particular of the so-called ESKAPE pathogens, urges the development of novel and innovative therapeutic approaches. Despite the antibiotic crisis rises, only one antibiotic with a novel mechanism of action has been approved in the last two decades. Although many innovative strategies to combat bacterial infections have been developed and resulted in promising bioactive substances, most drugs in clinical trials are still based on modifications of already approved drugs. Thus a revival of the golden age of antibiotics is still far away and also in near future enormous efforts are required for the development of efficient therapies.

In order to highlight the recent advances in the fight against bacterial infections, this special issue seeks manuscript submissions from all areas of antibacterial drug discovery. Topics may cover the discovery and validation of novel drug targets in pathogenic Gram-positive and Gram-negative bacteria, the identification of antibacterial compounds (small molecules, natural products, peptides and peptidomimetics, nanoparticles, and others) or adjuvants, assessments of treatment combinations, or the development of novel techniques and assays that support antibacterial drug discovery.

Dr. Björn Windshügel
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Antibiotics is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Published Papers (5 papers)

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Research

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10 pages, 1995 KiB  
Article
Apomorphine Targets the Pleiotropic Bacterial Regulator Hfq
by Florian Turbant, David Partouche, Omar El Hamoui, Sylvain Trépout, Théa Legoubey, Frank Wien and Véronique Arluison
Antibiotics 2021, 10(3), 257; https://doi.org/10.3390/antibiotics10030257 - 4 Mar 2021
Cited by 6 | Viewed by 1988
Abstract
Hfq is a bacterial regulator with key roles in gene expression. The protein notably regulates translation efficiency and RNA decay in Gram-negative bacteria, thanks to its binding to small regulatory noncoding RNAs. This property is of primary importance for bacterial adaptation and survival [...] Read more.
Hfq is a bacterial regulator with key roles in gene expression. The protein notably regulates translation efficiency and RNA decay in Gram-negative bacteria, thanks to its binding to small regulatory noncoding RNAs. This property is of primary importance for bacterial adaptation and survival in hosts. Small RNAs and Hfq are, for instance, involved in the response to antibiotics. Previous work has shown that the E. coli Hfq C-terminal region (Hfq-CTR) self-assembles into an amyloid structure. It was also demonstrated that the green tea compound EpiGallo Catechin Gallate (EGCG) binds to Hfq-CTR amyloid fibrils and remodels them into nonamyloid structures. Thus, compounds that target the amyloid region of Hfq may be used as antibacterial agents. Here, we show that another compound that inhibits amyloid formation, apomorphine, may also serve as a new antibacterial. Our results provide an alternative in order to repurpose apomorphine, commonly used in the treatment of Parkinson’s disease, as an antibiotic to block bacterial adaptation to treat infections. Full article
(This article belongs to the Special Issue Antibacterial Drug Discovery)
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8 pages, 2271 KiB  
Article
Screening of an FDA-Approved Library for Novel Drugs against Y. pestis
by David Gur, Theodor Chitlaru, Emanuelle Mamroud and Ayelet Zauberman
Antibiotics 2021, 10(1), 40; https://doi.org/10.3390/antibiotics10010040 - 3 Jan 2021
Cited by 1 | Viewed by 2465
Abstract
Yersinia pestis is a Gram-negative pathogen that causes plague, a devastating disease that kills millions worldwide. Although plague is efficiently treatable by recommended antibiotics, the time of antibiotic therapy initiation is critical, as high mortality rates have been observed if treatment is delayed [...] Read more.
Yersinia pestis is a Gram-negative pathogen that causes plague, a devastating disease that kills millions worldwide. Although plague is efficiently treatable by recommended antibiotics, the time of antibiotic therapy initiation is critical, as high mortality rates have been observed if treatment is delayed for longer than 24 h after symptom onset. To overcome the emergence of antibiotic resistant strains, we attempted a systematic screening of Food and Drug Administration (FDA)-approved drugs to identify alternative compounds which may possess antibacterial activity against Y. pestis. Here, we describe a drug-repurposing approach, which led to the identification of two antibiotic-like activities of the anticancer drugs bleomycin sulfate and streptozocin that have the potential for designing novel antiplague therapy approaches. The inhibitory characteristics of these two drugs were further addressed as well as their efficiency in affecting the growth of Y. pestis strains resistant to doxycycline and ciprofloxacin, antibiotics recommended for plague treatment. Full article
(This article belongs to the Special Issue Antibacterial Drug Discovery)
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17 pages, 2000 KiB  
Article
New Antimicrobial Bioactivity against Multidrug-Resistant Gram-Positive Bacteria of Kinase Inhibitor IMD0354
by Iliana E Escobar, Alexis White, Wooseong Kim and Eleftherios Mylonakis
Antibiotics 2020, 9(10), 665; https://doi.org/10.3390/antibiotics9100665 - 1 Oct 2020
Cited by 10 | Viewed by 3633
Abstract
Multidrug-resistant pathogens pose a serious threat to human health. For decades, the antibiotic vancomycin has been a potent option when treating Gram-positive multidrug-resistant infections. Nonetheless, in recent decades, we have begun to see an increase in vancomycin-resistant bacteria. Here, we show that the [...] Read more.
Multidrug-resistant pathogens pose a serious threat to human health. For decades, the antibiotic vancomycin has been a potent option when treating Gram-positive multidrug-resistant infections. Nonetheless, in recent decades, we have begun to see an increase in vancomycin-resistant bacteria. Here, we show that the nuclear factor-kappa B (NF-κB) inhibitor N-[3,5-Bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (IMD0354) was identified as a positive hit through a Caenorhabditis elegans–methicillin-resistant Staphylococcus aureus (MRSA) infection screen. IMD0354 was a potent bacteriostatic drug capable of working at a minimal inhibitory concentration (MIC) as low as 0.06 µg/mL against various vancomycin-resistant strains. Interestingly, IMD0354 showed no hemolytic activity at concentrations as high as 16 µg/mL and is minimally toxic to C. elegans in vivo with 90% survival up to 64 µg/mL. In addition, we demonstrated that IMD0354′s mechanism of action at high concentrations is membrane permeabilization. Lastly, we found that IMD0354 is able to inhibit vancomycin-resistant Staphylococcus aureus (VRSA) initial cell attachment and biofilm formation at sub-MIC levels and above. Our work highlights that the NF-κB inhibitor IMD0354 has promising potential as a lead compound and an antimicrobial therapeutic candidate capable of combating multidrug-resistant bacteria. Full article
(This article belongs to the Special Issue Antibacterial Drug Discovery)
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7 pages, 517 KiB  
Communication
Mersaquinone, A New Tetracene Derivative from the Marine-Derived Streptomyces sp. EG1 Exhibiting Activity against Methicillin-Resistant Staphylococcus aureus (MRSA)
by Min Cheol Kim, Reiko Cullum, Ali M. S. Hebishy, Hala A. Mohamed, Ahmed H. I. Faraag, Nehad M. Salah, Mohamed S. Abdelfattah and William Fenical
Antibiotics 2020, 9(5), 252; https://doi.org/10.3390/antibiotics9050252 - 14 May 2020
Cited by 22 | Viewed by 4547
Abstract
New antibiotics are desperately needed to overcome the societal challenges being encountered with methicillin-resistant Staphylococcus aureus (MRSA). In this study, a new tetracene derivative, named Mersaquinone (1), and the known Tetracenomycin D (2), Resistoflavin (3) and Resistomycin [...] Read more.
New antibiotics are desperately needed to overcome the societal challenges being encountered with methicillin-resistant Staphylococcus aureus (MRSA). In this study, a new tetracene derivative, named Mersaquinone (1), and the known Tetracenomycin D (2), Resistoflavin (3) and Resistomycin (4) have been isolated from the organic extract of the marine Streptomyces sp. EG1. The strain was isolated from a sediment sample collected from the North Coast of the Mediterranean Sea of Egypt. The chemical structure of Mersaquinone (1) was assigned based upon data from a diversity of spectroscopic techniques including HRESIMS, IR, 1D and 2D NMR measurements. Mersaquinone (1) showed antibacterial activity against methicillin-resistant Staphylococcus aureus with a minimum inhibitory concentration of 3.36 μg/mL. Full article
(This article belongs to the Special Issue Antibacterial Drug Discovery)
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Review

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73 pages, 675 KiB  
Review
Fosfomycin as Partner Drug for Systemic Infection Management. A Systematic Review of Its Synergistic Properties from In Vitro and In Vivo Studies
by Roberta Maria Antonello, Luigi Principe, Alberto Enrico Maraolo, Valentina Viaggi, Riccardo Pol, Massimiliano Fabbiani, Francesca Montagnani, Antonio Lovecchio, Roberto Luzzati and Stefano Di Bella
Antibiotics 2020, 9(8), 500; https://doi.org/10.3390/antibiotics9080500 - 10 Aug 2020
Cited by 35 | Viewed by 7517
Abstract
Fosfomycin is being increasingly prescribed for multidrug-resistant bacterial infections. In patients with systemic involvement, intravenous fosfomycin is usually administered as a partner drug, as part of an antibiotic regimen. Hence, the knowledge of fosfomycin pharmacodynamic interactions (synergistic, additive, indifferent and antagonistic effect) is [...] Read more.
Fosfomycin is being increasingly prescribed for multidrug-resistant bacterial infections. In patients with systemic involvement, intravenous fosfomycin is usually administered as a partner drug, as part of an antibiotic regimen. Hence, the knowledge of fosfomycin pharmacodynamic interactions (synergistic, additive, indifferent and antagonistic effect) is fundamental for a proper clinical management of severe bacterial infections. We performed a systematic review to point out fosfomycin’s synergistic properties, when administered with other antibiotics, in order to help clinicians to maximize drug efficacy optimizing its use in clinical practice. Interactions were more frequently additive or indifferent (65.4%). Synergism accounted for 33.7% of total interactions, while antagonism occurred sporadically (0.9%). Clinically significant synergistic interactions were mostly distributed in combination with penicillins (51%), carbapenems (43%), chloramphenicol (39%) and cephalosporins (33%) in Enterobactaerales; with linezolid (74%), tetracyclines (72%) and daptomycin (56%) in Staphylococcus aureus; with chloramphenicol (53%), aminoglycosides (43%) and cephalosporins (36%) against Pseudomonas aeruginosa; with daptomycin (97%) in Enterococcus spp. and with sulbactam (75%) and penicillins (60%) and in Acinetobacter spp. fosfomycin-based antibiotic associations benefit from increase in the bactericidal effect and prevention of antimicrobial resistances. Taken together, the presence of synergistic interactions and the nearly total absence of antagonisms, make fosfomycin a good partner drug in clinical practice. Full article
(This article belongs to the Special Issue Antibacterial Drug Discovery)
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