Special Issue "Novel Antibacterial Agents"

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: 31 October 2020.

Special Issue Editors

Prof. Dr. Fiorella Meneghetti
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Guest Editor
Università degli Studi di Milano, Department of Pharmaceutical Sciences, Milan, Italy
Interests: diffraction techniques; structure elucidation; conformation of bioactive compounds; antitubercular agents
Special Issues and Collections in MDPI journals
Prof. Dr. Daniela Barlocco
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Guest Editor
Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via L. Mangiagalli 25, 20133 Milano, Italy
Interests: protein–protein interaction inhibitors; enzyme inhibitors; multi-target drugs; anticancer agents
Special Issues and Collections in MDPI journals

Special Issue Information

Dear Colleagues,

Infectious diseases still account for a substantial proportion of deaths worldwide. The plague of antimicrobial resistance represents an alarming signal for both human and animal healthcare, which drives the search for novel classes of antibiotics to replenish our armamentarium against bacterial infections.There is a great interest in the opportunities and challenges associated with tackling infectious diseases for developing effective and possibly cheap antimicrobial agents endowed with new mechanisms of action. The discovery of new antimicrobials as well as the expansion of utility of existing antibiotics would be crucial to fight the ever-increasing antimicrobial resistance of “superbugs”, pathogenic fungi, viruses, and parasites. Pharmaceuticals invites both reviews and original articles highlighting the recent medicinal chemistry research on novel antibacterial agents. Topics include natural product screening, identification and validation of new antibacterial targets and strategies for the discovery and optimization of antibacterial compounds.

The collection of manuscripts will be published as a Special Issue of the journal.

Dr. Fiorella Meneghetti
Prof. Daniela Barlocco
Guest Editors

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 papers will be 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. Pharmaceuticals 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 1000 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

  • small molecules
  • peptides
  • peptidomimetics
  • bacterial infections
  • fungi
  • virus
  • parasites
  • drug design
  • computational tools
  • biology assays
  • resistance mechanisms.

Published Papers (2 papers)

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Research

Open AccessArticle
Products Derived from Buchenavia tetraphylla Leaves Have In Vitro Antioxidant Activity and Protect Tenebrio molitor Larvae against Escherichia coli-Induced Injury
Pharmaceuticals 2020, 13(3), 46; https://doi.org/10.3390/ph13030046 - 16 Mar 2020
Abstract
The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high antioxidant action from B. tetraphylla (BT) [...] Read more.
The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high antioxidant action from B. tetraphylla (BT) leaf extracts. In vitro methods (DPPH and ABTS assays; determination of phenolic and flavonoid contents) were used to select products derived from B. tetraphylla with high antioxidant action. Then, the samples with the highest potentials were evaluated in a model of injury based on the inoculation of a lethal dose of heat-inactivated Escherichia coli in Tenebrio molitor larvae. Due to its higher antioxidant properties, the methanolic extract (BTME) was chosen to be fractionated using Sephadex LH-20 column-based chromatography. Two fractions from BTME (BTFC and BTFD) were the most active fractions. Pre-treatment with these fractions protected larvae of T. molitor from the stress induced by inoculation of heat-inactivated E. coli. Similarly, BTFC and BTFD increased the lifespan of larvae infected with a lethal dose of enteroaggregative E. coli 042. NMR data indicated the presence of aliphatic compounds (terpenes, fatty acids, carbohydrates) and aromatic compounds (phenolic compounds). These findings suggested that products derived from B. tetraphylla leaves are promising candidates for the development of antioxidant and anti-infective agents able to treat oxidative-related dysfunctions. Full article
(This article belongs to the Special Issue Novel Antibacterial Agents)
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Open AccessArticle
In Vitro Assessment of Antimicrobial, Antioxidant, and Cytotoxic Properties of Saccharin–Tetrazolyl and –Thiadiazolyl Derivatives: The Simple Dependence of the pH Value on Antimicrobial Activity
Pharmaceuticals 2019, 12(4), 167; https://doi.org/10.3390/ph12040167 - 12 Nov 2019
Cited by 1
Abstract
The antimicrobial, antioxidant, and cytotoxic activities of a series of saccharin–tetrazolyl and –thiadiazolyl analogs were examined. The assessment of the antimicrobial properties of the referred-to molecules was completed through an evaluation of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values against [...] Read more.
The antimicrobial, antioxidant, and cytotoxic activities of a series of saccharin–tetrazolyl and –thiadiazolyl analogs were examined. The assessment of the antimicrobial properties of the referred-to molecules was completed through an evaluation of minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values against Gram-positive and Gram-negative bacteria and yeasts. Scrutiny of the MIC and MBC values of the compounds at pH 4.0, 7.0, and 9.0 against four Gram-positive strains revealed high values for both the MIC and MBC at pH 4.0 (ranging from 0.98 to 125 µg/mL) and moderate values at pH 7.0 and 9.0, exposing strong antimicrobial activities in an acidic medium. An antioxidant activity analysis of the molecules was performed by using the DPPH (2,2-diphenyl-1-picrylhydrazyl) method, which showed high activity for the TSMT (N-(1-methyl-2H-tetrazol-5-yl)-N-(1,1-dioxo-1,2-benzisothiazol-3-yl) amine, 7) derivative (90.29% compared to a butylated hydroxytoluene positive control of 61.96%). Besides, the general toxicity of the saccharin analogs was evaluated in an Artemia salina model, which displayed insignificant toxicity values. In turn, upon an assessment of cell viability, all of the compounds were found to be nontoxic in range concentrations of 0–100 µg/mL in H7PX glioma cells. The tested molecules have inspiring antimicrobial and antioxidant properties that represent potential core structures in the design of new drugs for the treatment of infectious diseases. Full article
(This article belongs to the Special Issue Novel Antibacterial Agents)
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