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Pharmaceuticals
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Small Molecules as Antimicrobials 2024
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Small Molecules as Antimicrobials 2024

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (15 December 2024) | Viewed by 1608

Special Issue Editor

Dr. Poce Giovanna

E-Mail Website
Guest Editor
Department of Chemistry and Technology of Drugs (DCTF), Sapienza University of Rome, Rome, Italy
Interests: medicinal chemistry; drug development; antimycobacterials; antibacterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The escalating threat of antimicrobial resistance and the continuous emergence of novel pathogens underscore the urgent need for innovative antimicrobial agents. This Special Issue, "Small Molecules as Antimicrobials", delves into the latest advancements and research breakthroughs in the development and application of small molecules to combat microbial infections. By focusing on small molecules, this Special Issue aims to highlight the versatility and potential of these compounds in addressing some of the most pressing challenges in infectious disease management. The insights gained from the featured studies are expected to pave the way for the development of next-generation antimicrobials that are more effective, less prone to resistance, and safer for clinical use.

This Special Issue will serve as a comprehensive resource for researchers, healthcare professionals, and policymakers dedicated to the fight against infectious diseases, offering a wealth of knowledge on the state of the art in small molecule antimicrobial research and development.

Potential topics include, but are not limited to, the following:

  • Reports on novel small molecules with potent antimicrobial activity discovered through various approaches, such as high-throughput screening, rational drug design, and natural product isolation.
  • Discussions on the optimization of lead compounds to enhance efficacy, reduce toxicity, and improve pharmacokinetic properties.
  • Research on advanced delivery systems for small molecule antimicrobials, including nanoparticles, liposomes, and targeted delivery methods to enhance bioavailability and reduce side effects.

Dr. Poce Giovanna
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. 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 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

  • small molecules
  • antimicrobials
  • antivirals
  • antibacterials
  • antimycobacterials

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (1 paper)

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Research

22 pages, 2761 KiB  
Article
New Benzofuran–Pyrazole-Based Compounds as Promising Antimicrobial Agents: Design, Synthesis, DNA Gyrase B Inhibition, and In Silico Studies
by Somaia S. Abd El-Karim, Manal M. Anwar, Yasmin M. Syam, Hassan M. Awad, Asmaa Negm El-Dein, Mohamed K. El-Ashrey, Hamad M. Alkahtani and Sameh H. Abdelwahed
Pharmaceuticals 2024, 17(12), 1664; https://doi.org/10.3390/ph17121664 - 10 Dec 2024
Cited by 1 | Viewed by 1288
Abstract
Background/Objectives: The alarming rise in antibiotic resistance necessitates the discovery of novel antimicrobial agents. This study aims to design, synthesize, and evaluate new benzofuran–pyrazole-based compounds for their antimicrobial, antioxidant, and anti-inflammatory properties. Methods: New benzofuran–pyrazole hybrid molecules were synthesized using the Vilsmeier–Haach reaction [...] Read more.
Background/Objectives: The alarming rise in antibiotic resistance necessitates the discovery of novel antimicrobial agents. This study aims to design, synthesize, and evaluate new benzofuran–pyrazole-based compounds for their antimicrobial, antioxidant, and anti-inflammatory properties. Methods: New benzofuran–pyrazole hybrid molecules were synthesized using the Vilsmeier–Haach reaction and other chemical processes. The structures of the synthesized compounds were confirmed through micro-analytical and spectral analyses. Their antimicrobial activities were assessed against various bacterial and fungal strains, while antioxidant and anti-inflammatory properties were evaluated using DPPH-free radical scavenging and HRBC membrane stabilization assays, respectively. The most promising compounds were further tested for DNA gyrase B inhibition. Results: Compounds 9, 10, and 11b–d exhibited significant broad-spectrum antimicrobial activity with MIC values ranging from 2.50 to 20 µg/mL. Compounds 4, 6, 9, 11b, and 11d demonstrated high antioxidant activity, with DPPH scavenging percentages between 84.16% and 90.52%. Most compounds showed substantial anti-inflammatory effects, with HRBC membrane stabilization percentages ranging from 86.70% to 99.25%. Compound 9 notably inhibited E. coli DNA gyrase B with an IC50 of 9.80 µM, comparable to ciprofloxacin. Conclusions: The benzofuran–pyrazole-based compounds, particularly compound 9, show great potential as new antimicrobial agents due to their broad-spectrum activity and potent DNA gyrase B inhibition. These findings support further development and optimization of these compounds for clinical applications. Full article
(This article belongs to the Special Issue Small Molecules as Antimicrobials 2024)
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