Discover New Antibiotics 2016

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

Deadline for manuscript submissions: closed (20 October 2016) | Viewed by 28233

Special Issue Editor

Department of Microbiology, University of Wisconsin-La Crosse, 1725 State St., La Crosse, WI 54601, USA
Interests: drug discovery; anti-staphylococcal drugs; bacterial pathogenesis; two-component systems; uropathogenic Escherichia coli
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

New drugs to treat infections are a subject of great concern. We are slowly losing the use of several classes of antibiotics to treat infections because of the advent of drug resistance. Novel drugs with unique mechanisms of action are needed to combat antibiotic resistance.

Several strategies are discussed on how to cope with this problem:
i) novel strategies being used to identify new antibiotics,
ii) an analysis of techniques being used to assess potential new antibiotics,
iii) elucidation of a new drug's mechanism of action,
iv) an assessment of what happens to a new antibiotic and where is goes in a mammalian system,
v) and determining the mechanisms responsible for resistance or persistence for a new antibiotic.

Antibiotics will publish a Special Issue focusing on the discovery of new antibiotics. It is my pleasure to invite submissions of high quality research based papers related to the topics mentioned above.

Prof. Dr. William R. Schwan
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

  • new strategies to find novel drugs
  • discovery of new drugs (isolation, drug characterization, and structure-function analysis)
  • determine a new drug's mechanism of action
  • determine the pharmacokinetic and pharmacodynamic properties of a new drug
  • assessment of resistance to a new drug

Published Papers (3 papers)

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Research

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3119 KiB  
Article
Docking into Mycobacterium tuberculosis Thioredoxin Reductase Protein Yields Pyrazolone Lead Molecules for Methicillin-Resistant Staphylococcus aureus
by Noreena L. Sweeney, Lauren Lipker, Alicia M. Hanson, Chris J. Bohl, Katie E. Engel, Kelsey S. Kalous, Mary E. Stemper, Daniel S. Sem and William R. Schwan
Antibiotics 2017, 6(1), 4; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics6010004 - 28 Jan 2017
Cited by 10 | Viewed by 5961
Abstract
The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus. [...] Read more.
The thioredoxin/thioredoxin reductase system (Trx/TrxR) is an attractive drug target because of its involvement in a number of important physiological processes, from DNA synthesis to regulating signal transduction. This study describes the finding of pyrazolone compounds that are active against Staphylococcus aureus. Initially, the project was focused on discovering small molecules that may have antibacterial properties targeting the Mycobacterium tuberculosis thioredoxin reductase. This led to the discovery of a pyrazolone scaffold-containing compound series that showed bactericidal capability against S. aureus strains, including drug-resistant clinical isolates. The findings support continued development of the pyrazolone compounds as potential anti-S. aureus antibiotics. Full article
(This article belongs to the Special Issue Discover New Antibiotics 2016)
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13081 KiB  
Article
The Search for Herbal Antibiotics: An In-Silico Investigation of Antibacterial Phytochemicals
by Mary Snow Setzer, Javad Sharifi-Rad and William N. Setzer
Antibiotics 2016, 5(3), 30; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics5030030 - 12 Sep 2016
Cited by 49 | Viewed by 11120
Abstract
Recently, the emergence and spread of pathogenic bacterial resistance to many antibiotics (multidrug-resistant strains) have been increasing throughout the world. This phenomenon is of great concern and there is a need to find alternative chemotherapeutic agents to combat these antibiotic-resistant microorganisms. Higher plants [...] Read more.
Recently, the emergence and spread of pathogenic bacterial resistance to many antibiotics (multidrug-resistant strains) have been increasing throughout the world. This phenomenon is of great concern and there is a need to find alternative chemotherapeutic agents to combat these antibiotic-resistant microorganisms. Higher plants may serve as a resource for new antimicrobials to replace or augment current therapeutic options. In this work, we have carried out a molecular docking study of a total of 561 antibacterial phytochemicals listed in the Dictionary of Natural Products, including 77 alkaloids (17 indole alkaloids, 27 isoquinoline alkaloids, 4 steroidal alkaloids, and 28 miscellaneous alkaloids), 99 terpenoids (5 monoterpenoids, 31 sesquiterpenoids, 52 diterpenoids, and 11 triterpenoids), 309 polyphenolics (87 flavonoids, 25 chalcones, 41 isoflavonoids, 5 neoflavonoids, 12 pterocarpans, 10 chromones, 7 condensed tannins, 11 coumarins, 30 stilbenoids, 2 lignans, 5 phenylpropanoids, 13 xanthones, 5 hydrolyzable tannins, and 56 miscellaneous phenolics), 30 quinones, and 46 miscellaneous phytochemicals, with six bacterial protein targets (peptide deformylase, DNA gyrase/topoisomerase IV, UDP-galactose mutase, protein tyrosine phosphatase, cytochrome P450 CYP121, and NAD+-dependent DNA ligase). In addition, 35 known inhibitors were docked with their respective targets for comparison purposes. Prenylated polyphenolics showed the best docking profiles, while terpenoids had the poorest. The most susceptible protein targets were peptide deformylases and NAD+-dependent DNA ligases. Full article
(This article belongs to the Special Issue Discover New Antibiotics 2016)
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Review

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1054 KiB  
Review
Thioridazine: A Non-Antibiotic Drug Highly Effective, in Combination with First Line Anti-Tuberculosis Drugs, against Any Form of Antibiotic Resistance of Mycobacterium tuberculosis Due to Its Multi-Mechanisms of Action
by Leonard Amaral and Miguel Viveiros
Antibiotics 2017, 6(1), 3; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics6010003 - 14 Jan 2017
Cited by 50 | Viewed by 10426
Abstract
This review presents the evidence that supports the use of thioridazine (TZ) for the therapy of a pulmonary tuberculosis infection regardless of its antibiotic resistance status. The evidence consists of in vitro and ex vivo assays that demonstrate the activity of TZ against [...] Read more.
This review presents the evidence that supports the use of thioridazine (TZ) for the therapy of a pulmonary tuberculosis infection regardless of its antibiotic resistance status. The evidence consists of in vitro and ex vivo assays that demonstrate the activity of TZ against all encountered Mycobacterium tuberculosis (Mtb) regardless of its antibiotic resistance phenotype, as well as in vivo as a therapy for mice infected with multi-drug resistant strains of Mtb, or for human subjects infected with extensively drug resistant (XDR) Mtb. The mechanisms of action by which TZ brings about successful therapeutic outcomes are presented in detail. Full article
(This article belongs to the Special Issue Discover New Antibiotics 2016)
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