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Antibiotics
Special Issues
Discovery and Design of New Antimicrobial Agents
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Discovery and Design of New Antimicrobial Agents

A special issue of Antibiotics (ISSN 2079-6382). This special issue belongs to the section "Novel Antimicrobial Agents".

Deadline for manuscript submissions: 31 December 2024 | Viewed by 912

Special Issue Editor

Dr. Jean Michel Brunel

E-Mail Website
Guest Editor
UMR_MD1, Faculté de Pharmacie, Aix-Marseille Universite, 27 Bd Jean Moulin, CEDEX 5, 13385 Marseille, France
Interests: antimicrobial agents; antibiotic enhancers; organic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The abuse of antibiotics has accelerated the phenomenon of antibiotic resistance and the discovery of new antimicrobials, as well as the expansion of utility of existing antibiotics, remains a priority to fight the ever-increasing antimicrobial resistance of “superbugs”, pathogenic fungi, etc. This Special Issue of Antibiotics entitled “Discovery and Design of New Antimicrobial Agents” will discuss the chemistry involved in the design and synthesis of original scaffolds, as well as biologically inspired molecules from nature. The structure–activity relationships of these molecules will be also examined to demonstrate the wide interest of chemists as well as biologists, marine scientists, and pharmacologists. The report of strategies to fight antimicrobial resistance by depicting original mechanisms of action against bacteria will be highlighted in this dedicated Special Issue.

Dr. Jean Michel Brunel
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

  • antimicrobial agents
  • fight resistance
  • new design
  • structure–activity relationships (SAR)

Published Papers (1 paper)

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Research

17 pages, 2774 KiB  
Article
Impact of Growth Conditions on High-Throughput Identification of Repurposing Drugs for Pseudomonas aeruginosa Cystic Fibrosis Lung Infections
by Giovanni Di Bonaventura, Veronica Lupetti and Arianna Pompilio
Antibiotics 2024, 13(7), 642; https://doi.org/10.3390/antibiotics13070642 - 12 Jul 2024
Viewed by 561
Abstract
Pseudomonas aeruginosa lung infections in cystic fibrosis (CF) patients represent a therapeutic challenge due to antibiotic resistance. Repurposing existing drugs is a promising approach for identifying new antimicrobials. A crucial factor in successful drug repurposing is using assay conditions that mirror the site [...] Read more.
Pseudomonas aeruginosa lung infections in cystic fibrosis (CF) patients represent a therapeutic challenge due to antibiotic resistance. Repurposing existing drugs is a promising approach for identifying new antimicrobials. A crucial factor in successful drug repurposing is using assay conditions that mirror the site of infection. Here, the impact of growth conditions on the anti-P. aeruginosa activity of a library of 3386 compounds was evaluated. To this, after 24 h exposure, the survival rate of CF P. aeruginosa RP73 planktonic cells was assessed spectrophotometrically under “CF-like” (artificial CF sputum, pH 6.8, 5% CO2) and enriched (Tryptone Soya Broth, pH 7.2, and aerobiosis) conditions. Among non-antibiotic compounds (n = 3127), 13.4% were active regardless of growth conditions, although only 3.2% had comparable activity; 4% and 6.2% were more active under CF-like or enriched conditions, respectively. Interestingly, 22.1% and 26.6% were active exclusively under CF-like and enriched conditions, respectively. Notably, 7 and 12 hits caused 100% killing under CF-like and enriched conditions, respectively. Among antibiotics (n = 234), 42.3% were active under both conditions, although only 18.4% showed comparable activity; 9.4% and 14.5% were more active under CF-like and enriched conditions, respectively. Interestingly, 23% and 16.6% were active exclusively under CF-like and enriched conditions, respectively. Sulphonamides showed higher activity under CF-like conditions, whereas tetracyclines, fluoroquinolones, and macrolides were more effective under enriched settings. Our findings indicated that growth conditions significantly affect the anti-P. aeruginosa activity of antibiotics and non-antibiotic drugs. Consequently, repurposing studies and susceptibility tests should be performed under physicochemical conditions that the pathogen tackles at the site of infection. Full article
(This article belongs to the Special Issue Discovery and Design of New Antimicrobial Agents)
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