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Design, Synthesis, and Biological Evaluation of Antimicrobial Agents

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 November 2023) | Viewed by 3100

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Guest Editor
Basic Sciences Department, Universidad del Bio Bio, Chillan, Chile
Interests: agricultural and biological sciences; pharmacology, toxicology and pharmaceutics; biochemistry, genetics and molecular biology; medicine; chemistry; chemical engineering; environmental science; materials science; health professions; neuroscience
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Special Issue Information

Dear Colleagues,

Antimicrobial resistance is one of the greatest challenges facing the world today. The COVID‑19 pandemic, caused by severe acute respiratory syndrome coronavirus 2, is a current example. Even though the number of drugs currently used in the clinical practice of infectious diseases is high, the identification of new antimicrobial agents and the improvement of new therapeutic strategies are urgently required.

This Special Issue focuses on plant-derived products and synthetic derivatives as antimicrobial agents. The submission of original articles, systematic reviews, short communications, and other types of articles on related topics are welcome. All manuscripts will follow standard journal peer-review practices, and those accepted for publication will appear in this Special Issue on the Design, Synthesis, and Biological Evaluation of Antimicrobial Agents. We look forward to receiving your contributions to this Special Issue.

Prof. Dr. Carlos L. Cespedes Acuña
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • plant extracts
  • plant-derived compounds
  • antibacterial activity
  • antifungal-activity-resistant strains
  • synthetic natural product derivatives
  • multidrug resistance

Published Papers (2 papers)

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Research

23 pages, 4574 KiB  
Article
Fungistatic Effect of Phthalide Lactones on Rhodotorula mucilaginosa
by Joanna Gach, Teresa Olejniczak, Jakub Pannek and Filip Boratyński
Molecules 2023, 28(14), 5423; https://doi.org/10.3390/molecules28145423 - 15 Jul 2023
Cited by 1 | Viewed by 1061
Abstract
Currently, there is an increasing number of cases of fungal infections caused by opportunistic strains of the yeast Rhodotorula mucilaginosa, mainly in immunocompromised patients during hospitalization. The excessive use of antibiotics and azole compounds increases the risk of resistance to microorganisms. A [...] Read more.
Currently, there is an increasing number of cases of fungal infections caused by opportunistic strains of the yeast Rhodotorula mucilaginosa, mainly in immunocompromised patients during hospitalization. The excessive use of antibiotics and azole compounds increases the risk of resistance to microorganisms. A new alternative to these drugs may be synthetic phthalide lactones with a structure identical to or similar to the natural ones found in celery plants, which show low toxicity and relatively high fungistatic activity. In the present study, the fungistatic activity of seven phthalide lactones was determined against R. mucilaginosa IHEM 18459. We showed that 3-n-butylidenephthalide, the most potent compound selected in the microdilution test, caused a dose-dependent decrease in dry yeast biomass. Phthalide accumulated in yeast cells and contributed to an increase in reactive oxygen species content. The synergistic effect of fluconazole resulted in a reduction in the azole concentration required for yeast inhibition. We observed changes in the color of the yeast cultures; thus, we conducted experiments to prove that the carotenoid profile was altered. The addition of lactones also triggered a decline in fatty acid methyl esters. Full article
(This article belongs to the Special Issue Design, Synthesis, and Biological Evaluation of Antimicrobial Agents)
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15 pages, 4494 KiB  
Article
Evaluation of Antimicrobial Activities against Various E. coli Strains of a Novel Hybrid Peptide—LENART01
by Pawel Serafin, Paweł Kowalczyk, Adriano Mollica, Azzurra Stefanucci, Anna K. Laskowska, Magdalena Zawadzka, Karol Kramkowski and Patrycja Kleczkowska
Molecules 2023, 28(13), 4955; https://doi.org/10.3390/molecules28134955 - 23 Jun 2023
Cited by 4 | Viewed by 1809
Abstract
Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains a difficult task. Indeed, there is an urgent need for innovation in the design and development of a microbial inhibitor. Given that many [...] Read more.
Finding the ideal antimicrobial drug with improved efficacy and a safety profile that eliminates antibiotic resistance caused by pathogens remains a difficult task. Indeed, there is an urgent need for innovation in the design and development of a microbial inhibitor. Given that many promising antimicrobial peptides with excellent broad-spectrum antibacterial properties are secreted by some frog species (e.g., bombesins, opioids, temporins, etc.), our goal was to identify the antimicrobial properties of amphibian-derived dermorphin and ranatensin peptides, which were combined to produce a hybrid compound. This new chimera (named LENART01) was tested for its antimicrobial activity against E. coli strains K12 and R1–R4, which are characterized by differences in lipopolysaccharide (LPS) core oligosaccharide structure. The results showed that LENART01 had superior activity against the R2 and R4 strains compared with the effects of the clinically available antibiotics ciprofloxacin or bleomycin (MIC values). Importantly, the inhibitory effect was not concentration dependent; however, LENART01 showed a time- and dose-dependent hemolytic effect in hemolytic assays. Full article
(This article belongs to the Special Issue Design, Synthesis, and Biological Evaluation of Antimicrobial Agents)
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