molecules-logo

Journal Browser

Journal Browser

The Medicinal Chemistry of Antibiotics

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

Deadline for manuscript submissions: closed (30 April 2020) | Viewed by 4245

Special Issue Editor


E-Mail Website
Guest Editor
Department of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, 881 Madison Avenue, Memphis, TN 38163, USA
Interests: anti-cancer drugs; antibiotics; antibacterial agents; bacterial infections; drug-resistant pathogens; medicinal chemistry; natural products; rational drug design; repurposing existing drugs and drug targets
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Infectious diseases accounted for high morbidity and mortality in the 19th century. Since the introduction of antibiotics and vaccines, millions of lives have been saved and life expectancy has rapidly increased. As a result, in industrial countries, diseases that are not transmissible (e.g., cardiovascular disease, cancer, and stroke) have been highlighted as the leading causes of death. The majority of antibacterial agents being applied in current clinical practices in infections were introduced in the period between the 1950s and 1980s. Lack of established treatment guidelines for drug-resistant bacterial infections and misuse of drugs that cause mutations in bacterial genomes have led to an increase in antibiotic resistance. Some bacteria have already acquired extensive drug (or pandrug) resistance. Although a different aspect, drug-resistant spore-forming Bacillus spp. are readily engineered to use as biological weapons. Therefore, multidrug-resistant bacteria are currently considered as an emergent global disease and a major public health problem, as well as a threat to world security (bioterrorism).
Despite the increase in antimicrobial resistance, the development of new antimicrobial agents is declining due in large part to the fact that research and development (R&D) in large pharmaceutical industries have leaned towards drug development for the leading chronic diseases in the last few decades. The continuous development of new antibacterial agents is essential to reduce the global threat of antibiotic resistance. Over the past 20 years, national governments (e.g., NIH/NIAID in the U.S.) and nonprofit organizations have assumed a critical role in supporting and stimulating private and public sectors to offer opportunities in the antibacterial drug market. Under the current research environment, antibacterial drug discovery has advanced to innovative translational sciences including target-oriented drug discovery, new organic syntheses, drug delivery approaches, and analytical and assay methods.
The aim of this Special Issue is to highlight the recent advances in antibacterial drug discovery. This Special Issue may include original research articles and reviews on drug targets, medicinal chemistry (structure–activity relationships), new chemical entities, natural products, novel assays, phage therapy, vaccines, computational chemistry, new formulations, drug delivery, pharmacokinetic and dynamic aspects, and new strategies to use approved drugs.

Prof. Dr. Michio Kurosu
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

  • antibacterial agents
  • medicinal chemistry
  • antibacterial drug discovery
  • antibacterial pharmacology
  • rational drug design of antibacterial agents
  • antibacterial drug delivery

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

9 pages, 1033 KiB  
Article
Antifungal Activity of Gentamicin B1 against Systemic Plant Mycoses
by Gaspar Banfalvi
Molecules 2020, 25(10), 2401; https://doi.org/10.3390/molecules25102401 - 21 May 2020
Cited by 6 | Viewed by 3587
Abstract
Background: Gentamicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora purpurea bacteria, effective against Gram-negative bacterial infections. Major fractions of the gentamicin complex (C1, C1a, C2, C2a) possess weak antifungal activity and one of the minor components (A, A1–A4, B, B1, X), gentamicin [...] Read more.
Background: Gentamicin is a broad-spectrum aminoglycoside antibiotic produced by Micromonospora purpurea bacteria, effective against Gram-negative bacterial infections. Major fractions of the gentamicin complex (C1, C1a, C2, C2a) possess weak antifungal activity and one of the minor components (A, A1–A4, B, B1, X), gentamicin B1 was found to be a strong antifungal agent. Methods: This work uses in vitro and in vivo dilution methods to compare the antifusarial, antiaspergillic and anticryptococcal effects of gentamicin derivatives and structurally-related congeners. Results: The in vitro antifusarial activity of gentamicin B1 (minimum inhibitory concentration (MIC) 0.4 μg/mL) and structurally-related compounds (MIC 0.8–12.5 μg/mL) suggests that the purpuroseamine ring substituents are responsible for the specific antimycotic effect. The functional groups of the garoseamine and 2-deoxystreptamine rings of gentamicin derivatives are identical in gentamicin compounds and are unlikely to exert a significant antifungal effect. Among soil dermatophytes, Microsporum gypseum was more susceptible to gentamicin B1 (MIC 3.1 µg/mL) than Trichophyton gypseum (MIC 25 µg/mL). The in vitro antifungal effect of gentamicin B1 against plant pathogenic fungi was comparable to primary antifungal agents. Conclusion: Gentamicin is already in medical use. In vitro and preclinical in vivo synergisms of gentamicin B1 with amphotericin B suggest immediate clinical trials starting with subtoxic doses. Full article
(This article belongs to the Special Issue The Medicinal Chemistry of Antibiotics)
Show Figures

Graphical abstract

Back to TopTop