New Methodologies of Antibiotic Therapy: Drug Design and Diagnostic Tools

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

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 6640

Special Issue Editors

Laboratory of Medicinal Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, and Institute of Biomedicine (IBUB), Barcelona, Spain
Interests: heterocyclic chemistry; multicomponent reactions; organic synthesis; medicinal chemistry
Instituto Universitario de Bio-Orgánica “Antonio González” (IUBO-AG), Universidad de La Laguna, C/Astrofísico Francisco Sánchez 2, 38206 La Laguna, Spain
Interests: anticancer compounds; drug discovery; drug design; phenotypic assays; mechanism of action; chemical databases
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Special Issue Information

Dear Colleagues,

Defeating infections is often described as the emerging challenge of the century. The search for novel, more efficient and safer antimicrobial agents is a constant social demand. On the one hand, with unprecedented infectious outbreaks, the alarming state of antibacterial resistance and growing environmental concerns regarding antibiotics, developing new scaffolds/compounds is of utmost importance. Moreover, due to the large number of affected populations, securing low-cost, green and convenient chemical production is crucial. Finally, as timely and precise diagnostics increase the success rate of treatments and control of infection spread, efficient tools and probes are also in high demand.

In this context, the present issue is willing to accept research and review papers that address the following:

  • Novel antimicrobial agents including small molecules, natural products, peptides, polymers and nanomaterials.
  • New synthetic strategies to conveniently access new/privileged scaffolds with antimicrobial activity and related libraries.
  • Novel diagnostic strategies based on (photo-, bio-, etc.) chemical probes.

Dr. Ouldouz Ghashghaei
Prof. Dr. José M. Padrón
Guest Editors

Manuscript Submission Information

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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
  • antibiotics
  • antivirals
  • natural products
  • small molecules
  • antimicrobial peptides
  • bioactive compounds
  • scaffolds
  • antimicrobial resistance
  • diagnostic methods and technologies
  • medicinal chemistry
  • preparative organic synthesis

Published Papers (3 papers)

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Research

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16 pages, 4671 KiB  
Article
Structures, Interactions and Activity of the N-Terminal Truncated Variants of Antimicrobial Peptide Thanatin
Antibiotics 2024, 13(1), 74; https://doi.org/10.3390/antibiotics13010074 - 12 Jan 2024
Cited by 1 | Viewed by 920
Abstract
Gram-negative bacteria are intrinsically more resistant to many frontline antibiotics, which is attributed to the permeability barrier of the outer membrane, drug efflux pumps and porins. Consequently, discovery of new small molecules antibiotics to kill drug-resistant Gram-negative bacteria presents a significant challenge. Thanatin, [...] Read more.
Gram-negative bacteria are intrinsically more resistant to many frontline antibiotics, which is attributed to the permeability barrier of the outer membrane, drug efflux pumps and porins. Consequently, discovery of new small molecules antibiotics to kill drug-resistant Gram-negative bacteria presents a significant challenge. Thanatin, a 21-residue insect-derived antimicrobial peptide, is known for its potent activity against Enterobacter Gram-negative bacteria, including drug-resistant strains. Here, we investigated a 15-residue N-terminal truncated analog PM15 (P1IIYCNRRTGKCQRM15) of thanatin to determine modes of action and antibacterial activity. PM15 and the P1 to Y and A substituted variants PM15Y and PM15A delineated interactions and permeabilization of the LPS–outer membrane. In antibacterial assays, PM15 and the analogs showed growth inhibition of strains of Gram-negative bacteria that is largely dependent on the composition of the culture media. Atomic-resolution structures of PM15 and PM15Y in free solution and in complex with LPS micelle exhibited persistent β-hairpin structures similar to native thanatin. However, in complex with LPS, the structures of peptides are more compact, with extensive packing interactions among residues across the two anti-parallel strands of the β-hairpin. The docked complex of PM15/LPS revealed a parallel orientation of the peptide that may be sustained by potential ionic and van der Waals interactions with the lipid A moiety of LPS. Further, PM15 and PM15Y bind to LptAm, a monomeric functional variant of LptA, the periplasmic component of the seven-protein (A-G) complex involved in LPS transport. Taken together, the structures, target interactions and antibacterial effect of PM15 presented in the current study could be useful in designing thanatin-based peptide analogs. Full article
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14 pages, 3551 KiB  
Article
Efficient AntiMycolata Agents by Increasing the Lipophilicity of Known Antibiotics through Multicomponent Reactions
Antibiotics 2023, 12(1), 83; https://doi.org/10.3390/antibiotics12010083 - 03 Jan 2023
Cited by 1 | Viewed by 2706
Abstract
New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against Mycolata bacteria. Microbiological guidance for medicinal chemistry is a powerful tool to design new and [...] Read more.
New antibiotic agents were prepared using Povarov and Ugi multicomponent reactions upon the known drugs sulfadoxine and dapsone. The prepared derivatives, with increased lipophilicity, showed improved efficiency against Mycolata bacteria. Microbiological guidance for medicinal chemistry is a powerful tool to design new and effective antimicrobials. In this case, the readily synthesized compounds open new possibilities in the search for antimicrobials active on mycolic acid-containing bacteria. Full article
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Review

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27 pages, 1080 KiB  
Review
Diagnosis by Microbial Culture, Breath Tests and Urinary Excretion Tests, and Treatments of Small Intestinal Bacterial Overgrowth
Antibiotics 2023, 12(2), 263; https://doi.org/10.3390/antibiotics12020263 - 28 Jan 2023
Cited by 4 | Viewed by 2540
Abstract
Small intestinal bacterial overgrowth (SIBO) is characterized as the increase in the number and/or alteration in the type of bacteria in the upper gastrointestinal tract and accompanies various bowel symptoms such as abdominal pain, bloating, gases, diarrhea, and so on. Clinically, SIBO is [...] Read more.
Small intestinal bacterial overgrowth (SIBO) is characterized as the increase in the number and/or alteration in the type of bacteria in the upper gastrointestinal tract and accompanies various bowel symptoms such as abdominal pain, bloating, gases, diarrhea, and so on. Clinically, SIBO is diagnosed by microbial culture in duodenum/jejunum fluid aspirates and/or the breath tests (BT) of hydrogen/methane gases after ingestion of carbohydrates such as glucose. The cultural analysis of aspirates is regarded as the golden standard for the diagnosis of SIBO; however, this is invasive and is not without risk to the patients. BT is an inexpensive and safe diagnostic test but lacks diagnostic sensitivity and specificity depending on the disease states of patients. Additionally, the urinary excretion tests are used for the SIBO diagnosis using chemically synthesized bile acid conjugates such as cholic acid (CA) conjugated with para-aminobenzoic acid (PABA-CA), ursodeoxycholic acid (UDCA) conjugated with PABA (PABA-UDCA) or conjugated with 5-aminosalicylic acid (5-ASA-UDCA). These conjugates are split by bacterial bile acid (cholylglycine) hydrolase. In the tests, the time courses of the urinary excretion rates of PABA or 5-ASA, including their metabolites, are determined as the measure of hydrolytic activity of intestinal bacteria. Although the number of clinical trials with this urinary excretion tests is small, results demonstrated the usefulness of bile acid conjugates as SIBO diagnostic substrates. PABA-UDCA disulfate, a single-pass type unabsorbable compound without the hydrolysis of conjugates, was likely to offer a simple and rapid method for the evaluation of SIBO without the use of radioisotopes or expensive special apparatus. Treatments of SIBO with antibiotics, probiotics, therapeutic diets, herbal medicines, and/or fecal microbiota transplantation are also reviewed. Full article
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