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Antibiotics
Special Issues
Design and Synthesis of Antimicrobial Compounds
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Design and Synthesis of 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 (29 February 2024) | Viewed by 6225

Special Issue Editors

Dr. Maria Marinescu

E-Mail Website
Guest Editor
Department of Organic Chemistry, Biochemistry and Catalysis, University of Bucharest, 90-92 Sos Panduril, RO-050663 Bucharest, Romania
Interests: syntheses of biologically active compounds; heterocycles (benzimidazoles, octahydroacridines, pyrimidines, pyrazoles); DFT; the correlation between the structure of the compounds and their antimicrobial activity; syntheses of compounds with nonlinear optical properties (NLO)
Dr. Christina Marie Zalaru

E-Mail Website
Guest Editor
Department of Organic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90-92 Panduri Street, 050663 Bucharest, Romania
Interests: synthesis; spectral characterization; anti-tumor activity of some pyrazole derivatives
Dr. George Dinos

E-Mail Website
Guest Editor
Laboratory of Biochemistry, School of Medicine, University of Patras, 26500 Patras, Greece
Interests: antibiotics; ribosome structure and function; protein biosynthesis; antibiotics development and evaluation; Chloramphenicol Derivatives
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Since the discovery and clinical application of penicillin, microbial natural products have played a critical role in protecting public health. However, the emergence and wide spread of drug-resistant pathogens pose a new grave threat to humankind and make it one of the world’s most severe public health problems. New chemical entries with antimicrobial activities, new mechanisms, or novel therapy methods are urgently needed for drug development. By exploring new sources, new technology in separation and structure elucidation, genome mining and synthetic biology, natural product research is entering a new golden age.

This Special Issue on natural products with antimicrobial activity will cover, though is not limited to, the discovery of new secondary metabolites, new mechanisms and new therapy methods related to potential applications in antimicrobial drug screening and development.

The synthesis, characterization and evaluation of the antimicrobial properties of organic or coordination compounds is the first step in realizing new antimicrobial agents. Bioinformatic analysis and the study of redox properties and reaction mechanisms help in understanding, redesigning and optimizing the characteristics of potential active molecules for fighting microorganisms (bacteria, fungi, and viruses).

At the moment, infection by the virus SARS-CoV-2 is a threat clearly perceived all over the world. Less widespread and broadcasted is the concern regarding microorganisms such as bacteria and fungi, especially for those with depleted immune systems. According to the European Centre for Disease Control, 3.8 million people acquire healthcare-associated infections and ca. 90,000 people die from them per year (data from 2018) in the EU.

The aim of this Special Issue is to put together relevant research on molecules that have the potential to contribute to reducing the number of fatalities caused by bacteria or fungi, as well as controlling microorganisms on agricultural crops and food.

Dr. Maria Marinescu
Dr. Christina Marie Zalaru
Dr. George Dinos
Guest Editors

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

  • synthesis
  • heterocyclic compounds
  • antimicrobial activity
  • antibiotic resistance
  • antimicrobial mechanisms
  • antibiotic targetsclinical applications
  • antibiotic development

Published Papers (3 papers)

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Research

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14 pages, 3996 KiB  
Article
Chloramphenicol Derivatization in Its Primary Hydroxyl Group with Basic Amino Acids Leads to New Pharmacophores with High Antimicrobial Activity
by Artemis Tsirogianni, Georgia G. Kournoutou, Maria Mpogiatzoglou, George Dinos and Constantinos M. Athanassopoulos
Antibiotics 2023, 12(5), 832; https://doi.org/10.3390/antibiotics12050832 - 29 Apr 2023
Viewed by 1610
Abstract
In a previous study published by our group, successful modification of the antibiotic chloramphenicol (CHL) was reported, which was achieved by replacing the dichloroacetyl tail with alpha and beta amino acids, resulting in promising new antibacterial pharmacophores. In this study, CHL was further [...] Read more.
In a previous study published by our group, successful modification of the antibiotic chloramphenicol (CHL) was reported, which was achieved by replacing the dichloroacetyl tail with alpha and beta amino acids, resulting in promising new antibacterial pharmacophores. In this study, CHL was further modified by linking the basic amino acids lysine, ornithine, and histidine to the primary hydroxyl group of CHL via triazole, carbamate, or amide bonding. Our results showed that while linking the basic amino acids retained antibacterial activity, it was somewhat reduced compared to CHL. However, in vitro testing demonstrated that all derivatives were comparable in activity to CHL and competed for the same ribosomal binding site with radioactive chloramphenicol. The amino acid–CHL tethering modes were evaluated either with carbamate (7, 8) derivatives, which exhibited higher activity, or with amide- (4–6) or triazole-bridged compounds (1–3), which were equally potent. Our findings suggest that these new pharmacophores have potential as antimicrobial agents, though further optimization is needed. Full article
(This article belongs to the Special Issue Design and Synthesis of Antimicrobial Compounds)
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19 pages, 6495 KiB  
Article
New Pyrazolo-Benzimidazole Mannich Bases with Antimicrobial and Antibiofilm Activities
by Christina Zalaru, Florea Dumitrascu, Constantin Draghici, Isabela Tarcomnicu, Maria Marinescu, George Mihai Nitulescu, Rodica Tatia, Lucia Moldovan, Marcela Popa and Mariana Carmen Chifiriuc
Antibiotics 2022, 11(8), 1094; https://doi.org/10.3390/antibiotics11081094 - 12 Aug 2022
Cited by 13 | Viewed by 1781
Abstract
A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized, characterized by 1H-NMR, 13C-NMR, IR, UV-Vis, MS, and elemental analysis. In vitro cytotoxicity of the new compounds studied on fibroblast cells showed that the newly synthesized pyrazolo-benzimidazole hybrid derivatives were noncytotoxic [...] Read more.
A new series of pyrazolo-benzimidazole hybrid Mannich bases were synthesized, characterized by 1H-NMR, 13C-NMR, IR, UV-Vis, MS, and elemental analysis. In vitro cytotoxicity of the new compounds studied on fibroblast cells showed that the newly synthesized pyrazolo-benzimidazole hybrid derivatives were noncytotoxic until the concentration of 1 μM and two compounds presented a high degree of biocompatibility. The antibacterial and antibiofilm activity of the newly synthesized compounds was assayed on Gram-positive Staphylococcus aureus ATCC25923, Enterococcus faecalis ATCC29212, and Gram-negative Pseudomonas aeruginosa ATCC27853, Escherichia coli ATCC25922 strains. All synthesized compounds 5a–g are more active against all three tested bacterial strains Staphylococcus aureus ATCC25923, Enterococcus faecalis ATCC29212, and Escherichia coli ATCC25922 than reference drugs (Metronidazole, Nitrofurantoin), with the exception of compounds 5d and 5g, which are less active compared to Nitrofurantoin, and all synthesized compounds 5a–g are more active against Pseudomonas aeruginosa ATCC27853 compared to reference drugs (Metronidazole, Nitrofurantoin). Compound 5f showed the best activity against Staphylococcus aureus ATCC 25923, with a MIC of 150 μg/mL and has also inhibited the biofilm formed by all the bacterial strains, having an MBIC of 310 µg/mL compared to the reference drugs (Metronidazole, Nitrofurantoin). Full article
(This article belongs to the Special Issue Design and Synthesis of Antimicrobial Compounds)
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Review

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39 pages, 18739 KiB  
Review
Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review
by Maria Marinescu
Antibiotics 2023, 12(7), 1220; https://doi.org/10.3390/antibiotics12071220 - 22 Jul 2023
Cited by 8 | Viewed by 2133
Abstract
Bacterial infections have attracted the attention of researchers in recent decades, especially due to the special problems they have faced, such as their increasing diversity and resistance to antibiotic treatment. The emergence and development of the SARS-CoV-2 infection stimulated even more research to [...] Read more.
Bacterial infections have attracted the attention of researchers in recent decades, especially due to the special problems they have faced, such as their increasing diversity and resistance to antibiotic treatment. The emergence and development of the SARS-CoV-2 infection stimulated even more research to find new structures with antimicrobial and antiviral properties. Among the heterocyclic compounds with remarkable therapeutic properties, benzimidazoles, and triazoles stand out, possessing antimicrobial, antiviral, antitumor, anti-Alzheimer, anti-inflammatory, analgesic, antidiabetic, or anti-ulcer activities. In addition, the literature of the last decade reports benzimidazole-triazole hybrids with improved biological properties compared to the properties of simple mono-heterocyclic compounds. This review aims to provide an update on the synthesis methods of these hybrids, along with their antimicrobial and antiviral activities, as well as the structure–activity relationship reported in the literature. It was found that the presence of certain groups grafted onto the benzimidazole and/or triazole nuclei (-F, -Cl, -Br, -CF3, -NO2, -CN, -CHO, -OH, OCH3, COOCH3), as well as the presence of some heterocycles (pyridine, pyrimidine, thiazole, indole, isoxazole, thiadiazole, coumarin) increases the antimicrobial activity of benzimidazole-triazole hybrids. Also, the presence of the oxygen or sulfur atom in the bridge connecting the benzimidazole and triazole rings generally increases the antimicrobial activity of the hybrids. The literature mentions only benzimidazole-1,2,3-triazole hybrids with antiviral properties. Both for antimicrobial and antiviral hybrids, the presence of an additional triazole ring increases their biological activity, which is in agreement with the three-dimensional binding mode of compounds. This review summarizes the advances of benzimidazole triazole derivatives as potential antimicrobial and antiviral agents covering articles published from 2000 to 2023. Full article
(This article belongs to the Special Issue Design and Synthesis of Antimicrobial Compounds)
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