Organic Synthesis of Drug-Like Antimicrobial Compounds

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

Deadline for manuscript submissions: closed (15 May 2024) | Viewed by 3026

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia, 020956 Bucharest, Romania
Interests: medicinal chemistry; organic synthesis; drug discovery

E-Mail Website
Guest Editor
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 6 Traian Vuia, 020956 Bucharest, Romania
Interests: medicinal chemistry; organic synthesis; drug discovery

Special Issue Information

Dear Colleagues,

Antimicrobials represent a crucial innovation in the field of medicine and possess the potential to significantly reducing the mortality and morbidity associated with infectious diseases. They have also played a pivotal role in advancing modern medicine, enabling procedures like transplantation, cancer chemotherapy, and surgery. Regrettably, the excessive and inappropriate use of antimicrobials in human medicine, as well as in agriculture and veterinary practices, has led to the emergence, proliferation, and spread of antimicrobial resistance (AMR). This is reflected in the alarming prevalence of antibiotic-resistant infections, accompanied by a rise in related mortality rates. In 2019, more than 33,000 patients in Europe lost their lives due to AMR; globally, this figure approached 1.2 million deaths.

The topic of AMR is further compounded by microbial biofilms, which exhibit significantly higher tolerance to antimicrobial agents compared to their planktonic counterparts, sometimes even reaching levels hundreds or thousands of times greater.

The emergence of bacterial infections and the spread of antimicrobial resistance have raised serious global concerns, necessitating urgent action to develop innovative and effective antibacterial strategies. One such approach involves continued efforts to incentivize the design and synthesis of new molecules as potential antimicrobial candidates.

Sharing the findings in this research field will undoubtedly contribute to better preparing the scientific community for the potential challenges of the so-called "post-antibiotic era."

Prof. Dr. Diana Camelia Nuta
Prof. Dr. Carmen Limban
Guest Editors

Manuscript Submission Information

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Keywords

  • synthesis
  • antimicrobial activity
  • antibacterial
  • antibiofilm
  • microbial resistance

Published Papers (2 papers)

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Research

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16 pages, 6362 KiB  
Article
Antimicrobial Activity of Novel Ni(II) and Zn(II) Complexes with (E)-2-((5-Bromothiazol-2-yl)imino)methyl)phenol Ligand: Synthesis, Characterization and Molecular Docking Studies
by Inas Al-Qadsy, Waseem Sharaf Saeed, Ahmad Abdulaziz Al-Owais, Abdelhabib Semlali, Ali Alrabie, Lena Ahmed Saleh Al-Faqeeh, Mohammed ALSaeedy, Arwa Al-Adhreai, Abdel-Basit Al-Odayni and Mazahar Farooqui
Antibiotics 2023, 12(11), 1634; https://doi.org/10.3390/antibiotics12111634 - 17 Nov 2023
Cited by 1 | Viewed by 1328
Abstract
In order to address the challenges associated with antibiotic resistance by bacteria, two new complexes, Ni(II) and Zn(II), have been synthesized using the conventional method based on Schiff base ligand (E)-2-((5-bromothiazol-2-yl) imino) methyl) phenol. The Schiff base ligand (HL) was synthesized using salicylaldehyde [...] Read more.
In order to address the challenges associated with antibiotic resistance by bacteria, two new complexes, Ni(II) and Zn(II), have been synthesized using the conventional method based on Schiff base ligand (E)-2-((5-bromothiazol-2-yl) imino) methyl) phenol. The Schiff base ligand (HL) was synthesized using salicylaldehyde and 5-(4-bromophenyl)thiazol-2-amine in both traditional and efficient, ecologically friendly, microwave-assisted procedures. The ligand and its complexes were evaluated by elemental analyses, FTIR spectroscopy, UV-Vis spectroscopy, nuclear magnetic resonance (NMR), thermogravimetric analysis (TGA) and magnetic susceptibility. The ligand and its complexes were tested for antibacterial activity against three Gram-positive bacteria (Staphylococcus aureus ATCC 25923, Methicillin-resistant Staphylococcus aureus ATCC 43300 and Enterococcus faecalis ATCC 29212) and three Gram-negative bacteria (Pseudomonas aeruginosa ATCC 27853, Escherichia coli ATCC 25922 and Klebsiella pneumoniae ATCC 700603). The findings demonstrate the potent activity of the ligand and its complexes against selective bacteria but the Ni(II) complex with MIC values ranging from 1.95 to 7.81 µg/mL outperformed all other compounds, including the widely used antibiotic Streptomycin. Furthermore, the docking study provided evidence supporting the validity of the antimicrobial results, since the Ni complex showed superior binding affinity against to E. coli NAD synthetase, which had a docking score (−7.61 kcal/mol). Full article
(This article belongs to the Special Issue Organic Synthesis of Drug-Like Antimicrobial Compounds)
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Review

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32 pages, 15808 KiB  
Review
Small Schiff Base Molecules—A Possible Strategy to Combat Biofilm-Related Infections
by Maria Coandă, Carmen Limban and Diana Camelia Nuță
Antibiotics 2024, 13(1), 75; https://doi.org/10.3390/antibiotics13010075 - 12 Jan 2024
Cited by 2 | Viewed by 1387
Abstract
Microorganisms participating in the development of biofilms exhibit heightened resistance to antibiotic treatment, therefore infections involving biofilms have become a problem in recent years as they are more difficult to treat. Consequently, research efforts are directed towards identifying novel molecules that not only [...] Read more.
Microorganisms participating in the development of biofilms exhibit heightened resistance to antibiotic treatment, therefore infections involving biofilms have become a problem in recent years as they are more difficult to treat. Consequently, research efforts are directed towards identifying novel molecules that not only possess antimicrobial properties but also demonstrate efficacy against biofilms. While numerous investigations have focused on antimicrobial capabilities of Schiff bases, their potential as antibiofilm agents remains largely unexplored. Thus, the objective of this article is to present a comprehensive overview of the existing scientific literature pertaining to small molecules categorized as Schiff bases with antibiofilm properties. The survey involved querying four databases (Web of Science, ScienceDirect, Scopus and Reaxys). Relevant articles published in the last 10 years were selected and categorized based on the molecular structure into two groups: classical Schiff bases and oximes and hydrazones. Despite the majority of studies indicating a moderate antibiofilm potential of Schiff bases, certain compounds exhibited a noteworthy effect, underscoring the significance of considering this type of molecular modeling when seeking to develop new molecules with antibiofilm effects. Full article
(This article belongs to the Special Issue Organic Synthesis of Drug-Like Antimicrobial Compounds)
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