Strategies for the Design of Hybrid-Based Antimicrobial Compounds

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

Deadline for manuscript submissions: 20 September 2025 | Viewed by 852

Special Issue Editors


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Department of Chemistry, Faculty of Science and Agriculture, University of Fort Hare, Alice 5700, South Africa
Interests: natural product chemistry; organic synthesis; hybrid compounds; antimicrobial compounds; anticancer compounds; phytochemicals and their derivatives; medicinal chemistry

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Department of Chemistry, Nelson Mandela University, P.O. Box 77000, Port Elizabeth 6001, South Africa
Interests: polymers; nanoparticles; wound dressings; skin regeneration; nanofibers; membranes; hydrogels; essential oils; anticancer drugs; antimalarials
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Guest Editor
Department of Chemistry, University of Fort Hare, Alice Campus, Alice 5700, South Africa
Interests: polymer-based materials; wound dressings; drug delivery systems; nanocarriers; drug discovery and design; organic synthesis of drug molecules (antimalarials, antimicrobials, anticancer)
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Special Issue Information

Dear Colleagues,

The need for innovative therapeutic strategies to enhance patient outcomes has increased due to the rising threat of multidrug-resistant (MDR) pathogens. In the design of antimicrobial drugs, hybrid molecules containing two or more pharmacophores have emerged as a promising drug design strategy to overcome the issue of MDR. These hybrid molecules display high potential to offer better pharmacokinetic characteristics, suppress resistance mechanisms, and enhance therapeutic outcomes.

The aim of this Special Issue is to provide a platform for researchers working on the synthesis, pharmacological evaluation, and mechanistic investigations of synthetic or plant-based hybrid antimicrobial drugs to publish their findings. Authors are invited to contribute their original research articles, reviews, and communications focusing on innovative hybrid molecules targeting bacterial, fungal, and viral infections.

Dr. Vuyolwethu Khwaza
Dr. Sibusiso Alven
Prof. Dr. Blessing Atim Aderibigbe
Guest Editors

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Keywords

  • hybrid compounds
  • antimicrobial agents
  • antibacterial agents
  • antifungal activity
  • antiviral activity
  • in vitro evaluation
  • structure–activity relationship (SAR)
  • bioactive molecules
  • nanoformulations
  • targeted drug delivery
  • pharmacological screening
  • clinical studies

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Published Papers (1 paper)

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Research

23 pages, 506 KiB  
Article
Design and Synthesis of Hybrid Compounds for Potential Treatment of Bacterial Co-Infections: In Vitro Antibacterial and In Silico Studies
by Vuyolwethu Khwaza, Opeoluwa O. Oyedeji, Eric Morifi, Mutshinyalo Nwamadi, Thierry Youmbi Fonkui, Derek Tantoh Ndinteh and Blessing A. Aderibigbe
Antibiotics 2025, 14(6), 582; https://doi.org/10.3390/antibiotics14060582 - 6 Jun 2025
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Abstract
Background: The need for innovative therapeutic strategies to enhance patient outcomes has increased due to the rise in bacterial co-infections associated with COVID-19. Methods: In this study, ten hybrid compounds were synthesized by combining two known pharmaceutical scaffolds to enhance antibacterial activity and [...] Read more.
Background: The need for innovative therapeutic strategies to enhance patient outcomes has increased due to the rise in bacterial co-infections associated with COVID-19. Methods: In this study, ten hybrid compounds were synthesized by combining two known pharmaceutical scaffolds to enhance antibacterial activity and overcome resistance mechanisms. The synthesized compounds were evaluated for their antibacterial activity against five Gram-negative and seven Gram-positive bacterial strains. In silico pharmacokinetic and drug-likeness properties of selected active compounds (1216, 19, 21, and 23) were predicted using the SwissADME web tool. Results: Compounds 12–16, 19, 21, and 23 demonstrated significant antibacterial activity, with compound 16 (a ciprofloxacin-containing hybrid) exhibiting the most potent effect, showing a minimum inhibitory concentration (MIC) of 7.8125 µg/mL against all tested bacterial strains. The in silico analysis revealed favorable pharmacokinetic profiles, drug-likeness, lipophilicity, and water solubility of most hybrid compounds. Discussion: The synthesized hybrid compounds exhibited enhanced antibacterial activity and desirable pharmacokinetic properties, particularly compound 16. These findings suggest the potential of these molecules in combating bacterial pathogens, especially those implicated in co-infections in COVID-19 infections. Conclusions: The study presents promising hybrid antibacterial agents with potential application as adjunct therapies for treating COVID-19-associated bacterial co-infections. Further investigation is needed, which may lead to effective treatments for managing secondary bacterial infections in viral disease contexts. Full article
(This article belongs to the Special Issue Strategies for the Design of Hybrid-Based Antimicrobial Compounds)
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