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Antibiotics
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Antibiotic Synthesis
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Antibiotic Synthesis

A special issue of Antibiotics (ISSN 2079-6382).

Deadline for manuscript submissions: closed (31 May 2017) | Viewed by 52812

Special Issue Editor

Prof. Dr. Naresh Kumar

E-Mail Website
Guest Editor
School of Chemistry, University of New South Wales, Sydney, NSW 2052, Australia
Interests: biologically active molecules; medicinal chemistry; organic chemical synthesis; peptidomimetics; novel antimicrobials; biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Bacterial infections are becoming increasingly problematic due to the increased incidence of drug-resistant pathogens, particularly in clinical settings. The long-term overuse and misuse of broad-spectrum antibiotics have greatly accelerated the development of this resistance. Furthermore, the “innovation gap” in the development of novel classes of antibiotics is becoming increasingly large.

Several strategies to combat this problem are discussed:

i)   The synthesis of new classes of compounds with antimicrobial activity;
ii)  Targeting new pathways for the development of antibiotics with reduced capacity to engender resistance;
iii) Identifying natural products with antimicrobial activity and developing their synthetic analogues;
iv)  Developing new methods for the targeted delivery of antibiotics;
v)   The synthetic modification of existing antibiotics to overcome resistance;
vi)  Dual-action and hybrid antibiotics.

Antibiotics will publish a Special Issue focusing on the discovery and development of new classes of antibiotic compounds, as well as novel molecular targets with reduced capacity to develop antibiotic resistance. It is my pleasure to invite submissions of high quality research-based papers related to the topics mentioned above.

Prof. Naresh Kumar
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.

Keywords

  • Discovery of new classes of antibiotics
  • Synthesis of antibiotic, anti-virulence and anti-biofilm compounds
  • Identification of new molecular targets
  • Development of methods for the targeted delivery of antibiotics

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Published Papers (7 papers)

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Research

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1728 KiB  
Article
Comparative Study on Antistaphylococcal Activity of Lipopeptides in Various Culture Media
by Maciej Jaśkiewicz, Damian Neubauer and Wojciech Kamysz
Antibiotics 2017, 6(3), 15; https://doi.org/10.3390/antibiotics6030015 - 2 Aug 2017
Cited by 11 | Viewed by 6283
Abstract
Staphylococcus aureus bacteria are one of the leading microorganisms responsible for nosocomial infections as well as being the primary causative pathogen of skin and wound infections. Currently, the therapy of staphylococcal diseases faces many difficulties, due to a variety of mechanisms of resistance [...] Read more.
Staphylococcus aureus bacteria are one of the leading microorganisms responsible for nosocomial infections as well as being the primary causative pathogen of skin and wound infections. Currently, the therapy of staphylococcal diseases faces many difficulties, due to a variety of mechanisms of resistance and virulence factors. Moreover, a number of infections caused by S. aureus are connected with biofilm formation that impairs effectiveness of the therapy. Short cationic lipopeptides that are designed on the basis of the structure of antimicrobial peptides are likely to provide a promising alternative to conventional antibiotics. Many research groups have proved a high antistaphylococcal potential of lipopeptides, however, the use of different protocols for determination of antimicrobial activity may be the reason for inconsistency of the results. The aim of this study was to learn how the use of various bacteriological media as well as solvents may affect activity of lipopeptides and their cyclic analogs. Obtained results showed a great impact of these variables. For example, cyclic analogs were more effective when dissolved in an aqueous solution of acetic acid and bovine serum albumin (BSA). The greater activity against planktonic cultures was found in brain-heart infusion broth (BHI) and tryptic-soy broth (TSB), while the antibiofilm activity was higher in the Mueller-Hinton medium. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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694 KiB  
Article
Antibacterial Activity and Toxicity of Analogs of Scorpion Venom IsCT Peptides
by Roberto De la Salud Bea, Adam F. Petraglia, Michael R. Ascuitto and Quentin M. Buck
Antibiotics 2017, 6(3), 13; https://doi.org/10.3390/antibiotics6030013 - 28 Jun 2017
Cited by 19 | Viewed by 4981
Abstract
Seven analogs of the natural, α-helix peptides IsCT1 and IsCT2—found in the venom of scorpion Opithancatus Madagascariensis—have been synthesized and tested to compare their antibacterial and hemolytic activity against natural peptides. In general, results show that increasing hydrophobicity by substituting positions 5 [...] Read more.
Seven analogs of the natural, α-helix peptides IsCT1 and IsCT2—found in the venom of scorpion Opithancatus Madagascariensis—have been synthesized and tested to compare their antibacterial and hemolytic activity against natural peptides. In general, results show that increasing hydrophobicity by substituting positions 5 and 9 of the sequences with alanine, valine, and leucine, enhances antibacterial activity. However, this also increases hemolytic activity. The analog with an increased net positive charge from +1 to +3 produces moderate bacterial growth inhibition but also has high hemolytic activity. On the other hand, the analog with a negative net charge (−1) has low antibacterial properties but also no cytotoxicity under the tested conditions, a similar result was found for five of the seven studied analogs. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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2183 KiB  
Article
Erythromycin Modification That Improves Its Acidic Stability while Optimizing It for Local Drug Delivery
by Erika L. Cyphert, Jaqueline D. Wallat, Jonathan K. Pokorski and Horst A. Von Recum
Antibiotics 2017, 6(2), 11; https://doi.org/10.3390/antibiotics6020011 - 25 Apr 2017
Cited by 51 | Viewed by 12565
Abstract
The antibiotic erythromycin has limited efficacy and bioavailability due to its instability and conversion under acidic conditions via an intramolecular dehydration reaction. To improve the stability of erythromycin, several analogs have been developed—such as azithromycin and clarithromycin—which decrease the rate of intramolecular dehydration. [...] Read more.
The antibiotic erythromycin has limited efficacy and bioavailability due to its instability and conversion under acidic conditions via an intramolecular dehydration reaction. To improve the stability of erythromycin, several analogs have been developed—such as azithromycin and clarithromycin—which decrease the rate of intramolecular dehydration. We set out to build upon this prior work by developing a conjugate of erythromycin with improved pH stability, bioavailability, and preferential release from a drug delivery system directly at the low pH of an infection site. To develop this new drug conjugate, adamantane-1-carbohydrazide was covalently attached to erythromycin via a pH-degradable hydrazone bond. Since Staphylococcus aureus infection sites are slightly acidic, the hydrazone bond will undergo hydrolysis liberating erythromycin directly at the infection site. The adamantane group provides interaction with the drug delivery system. This local delivery strategy has the potential of reducing off-target and systemic side-effects. This work demonstrates the synthesis of a pH-cleavable, erythromycin conjugate that retains the inherent antimicrobial activity of erythromycin, has an increased hydrophobicity, and improved stability in acidic conditions; thereby enhancing erythromycin’s bioavailability while simultaneously reducing its toxicity. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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4430 KiB  
Article
Final Demonstration of the Co-Identity of Lipiarmycin A3 and Tiacumicin B (Fidaxomicin) through Single Crystal X-ray Analysis
by Stefano Serra, Luciana Malpezzi, Angelo Bedeschi, Claudio Fuganti and Piera Fonte
Antibiotics 2017, 6(1), 7; https://doi.org/10.3390/antibiotics6010007 - 8 Feb 2017
Cited by 18 | Viewed by 6643
Abstract
Lipiarmycin A3 and tiacumicin B possess the same chemical structure and have been considered identical till recently, when some authors have suggested the possibility of a minor difference between the chemical structures of the two antibiotics. In this work we performed a comparative [...] Read more.
Lipiarmycin A3 and tiacumicin B possess the same chemical structure and have been considered identical till recently, when some authors have suggested the possibility of a minor difference between the chemical structures of the two antibiotics. In this work we performed a comparative X-ray analysis of lipiarmycin A3 and tiacumicin B. Although the commercial samples of the aforementioned compounds crystallize into two different crystal systems—evidently due to the different crystallization conditions—their chemical structures are identical. These results confirmed the previous assigned chemical structure of lipiarmycin A3 and its absolute configuration as well as its co-identity with the chemical structure of tiacumicin B, providing the definitive proof that these pharmaceutical compounds are identical in all respects. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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1283 KiB  
Article
Fused-Ring Oxazolopyrrolopyridopyrimidine Systems with Gram-Negative Activity
by Yiyuan Chen, Jonathan G. Moloney, Kirsten E. Christensen and Mark G. Moloney
Antibiotics 2017, 6(1), 2; https://doi.org/10.3390/antibiotics6010002 - 13 Jan 2017
Cited by 8 | Viewed by 5155
Abstract
Fused polyheterocyclic derivatives are available by annulation of a tetramate scaffold, and been shown to have antibacterial activity against a Gram-negative, but not a Gram-positive, bacterial strain. While the activity is not potent, these systems are structurally novel showing, in particular, a high [...] Read more.
Fused polyheterocyclic derivatives are available by annulation of a tetramate scaffold, and been shown to have antibacterial activity against a Gram-negative, but not a Gram-positive, bacterial strain. While the activity is not potent, these systems are structurally novel showing, in particular, a high level of polarity, and offer potential for the optimization of antibacterial activity. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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Review

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2124 KiB  
Review
Macromolecular Conjugate and Biological Carrier Approaches for the Targeted Delivery of Antibiotics
by Nhan Dai Thien Tram and Pui Lai Rachel Ee
Antibiotics 2017, 6(3), 14; https://doi.org/10.3390/antibiotics6030014 - 4 Jul 2017
Cited by 9 | Viewed by 7389
Abstract
For the past few decades, the rapid rise of antibiotic multidrug-resistance has presented a palpable threat to human health worldwide. Meanwhile, the number of novel antibiotics released to the market has been steadily declining. Therefore, it is imperative that we utilize innovative approaches [...] Read more.
For the past few decades, the rapid rise of antibiotic multidrug-resistance has presented a palpable threat to human health worldwide. Meanwhile, the number of novel antibiotics released to the market has been steadily declining. Therefore, it is imperative that we utilize innovative approaches for the development of antimicrobial therapies. This article will explore alternative strategies, namely drug conjugates and biological carriers for the targeted delivery of antibiotics, which are often eclipsed by their nanomedicine-based counterparts. A variety of macromolecules have been investigated as conjugate carriers, but only those most widely studied in the field of infectious diseases (e.g., proteins, peptides, antibodies) will be discussed in detail. For the latter group, blood cells, especially erythrocytes, have been successfully tested as homing carriers of antimicrobial agents. Bacteriophages have also been studied as a candidate for similar functions. Once these alternative strategies receive the amount of research interest and resources that would more accurately reflect their latent applicability, they will inevitably prove valuable in the perennial fight against antibiotic resistance. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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3745 KiB  
Review
Biotin Protein Ligase Is a Target for New Antibacterials
by Jiage Feng, Ashleigh S. Paparella, Grant W. Booker, Steven W. Polyak and Andrew D. Abell
Antibiotics 2016, 5(3), 26; https://doi.org/10.3390/antibiotics5030026 - 25 Jul 2016
Cited by 22 | Viewed by 8661
Abstract
There is a desperate need for novel antibiotic classes to combat the rise of drug resistant pathogenic bacteria, such as Staphylococcus aureus. Inhibitors of the essential metabolic enzyme biotin protein ligase (BPL) represent a promising drug target for new antibacterials. Structural and [...] Read more.
There is a desperate need for novel antibiotic classes to combat the rise of drug resistant pathogenic bacteria, such as Staphylococcus aureus. Inhibitors of the essential metabolic enzyme biotin protein ligase (BPL) represent a promising drug target for new antibacterials. Structural and biochemical studies on the BPL from S. aureus have paved the way for the design and development of new antibacterial chemotherapeutics. BPL employs an ordered ligand binding mechanism for the synthesis of the reaction intermediate biotinyl-5′-AMP from substrates biotin and ATP. Here we review the structure and catalytic mechanism of the target enzyme, along with an overview of chemical analogues of biotin and biotinyl-5′-AMP as BPL inhibitors reported to date. Of particular promise are studies to replace the labile phosphoroanhydride linker present in biotinyl-5′-AMP with alternative bioisosteres. A novel in situ click approach using a mutant of S. aureus BPL as a template for the synthesis of triazole-based inhibitors is also presented. These approaches can be widely applied to BPLs from other bacteria, as well as other closely related metabolic enzymes and antibacterial drug targets. Full article
(This article belongs to the Special Issue Antibiotic Synthesis)
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