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Molecules
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Novel Antimicrobial Agents: Design, Synthesis and Activity
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Novel Antimicrobial Agents: Design, Synthesis and Activity

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 June 2023) | Viewed by 10629

Special Issue Editors

Dr. Peng Teng

E-Mail Website
Guest Editor
College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China
Interests: medicinal chemistry; drug design; peptide-based drug; carbohydrate research
Dr. Chao Lu

E-Mail Website
Guest Editor
College of Pharmacy, Jinan University, Guangzhou, China
Interests: membrane-active peptides/peptidomimetics; smarted drug delivery system; microneedles; hydrogel; nanosheets; bioinspired materials; biomaterials
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The discovery of antibiotics has improved human health significantly; however, the global increase of antibiotic resistance has compromised the usefulness of antibiotics recently. In addition, the steady decline in the discovery of new antibiotics exacerbates the problem of multidrug resistance. No new class of antibiotics for the treatment of Gram-negative bacteria has been approved in the last four decades. Hence, there is an urgent need for the development of new types of antibiotics against multidrug-resistant bacteria.

While the major efforts have been focused on the structural modification of existing antibiotic classes, some new targets or mechanisms of action have emerged recently as therapeutically strategies to tackle the clinically relevant resistance. The Special Issue “Novel Antimicrobial Agents: Design, Synthesis, and Activity” aims to present the recent achievements in the rational design and synthesis of new antimicrobial agents in terms of new chemical scaffolds, to expand the limited structural diversity. Typically, new cyclic lipopeptides, antimicrobial peptide mimics, and new class of small-molecules stand for the highest potential toolbox to reinvigorate the discovery of new antibiotics. In addition, the antimicrobial activities and resistance profiles of newly obtained compounds against both Gram-positive and Gram-negative bacterial pathogens will be covered concomitantly. Both research articles and review papers will be included in this particular topic.

Dr. Peng Teng
Dr. Chao Lu
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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 agents
  • multidrug resistance
  • antibiotic-resistant pathogen
  • drug discovery
  • structural diversity
  • antimicrobial peptides

Published Papers (5 papers)

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Research

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11 pages, 1485 KiB  
Article
In Vitro Anti-Microbial Activity and Anti-Cancer Potential of Novel Synthesized Carbamothioyl-Furan-2-Carboxamide Derivatives
by Muhammad Salman Javed, Muhammad Zubair, Komal Rizwan and Muhammad Jamil
Molecules 2023, 28(12), 4583; https://doi.org/10.3390/molecules28124583 - 06 Jun 2023
Cited by 1 | Viewed by 1113
Abstract
A series of carbamothioyl-furan-2-carboxamide derivatives were synthesized using a one-pot strategy. Compounds were obtained in moderate to excellent yields (56–85%). Synthesized derivatives were evaluated for their anti-cancer (HepG2, Huh-7, and MCF-7 human cancer cell lines) and anti-microbial potential. Compound p-tolylcarbamothioyl)furan-2-carboxamide showed the highest [...] Read more.
A series of carbamothioyl-furan-2-carboxamide derivatives were synthesized using a one-pot strategy. Compounds were obtained in moderate to excellent yields (56–85%). Synthesized derivatives were evaluated for their anti-cancer (HepG2, Huh-7, and MCF-7 human cancer cell lines) and anti-microbial potential. Compound p-tolylcarbamothioyl)furan-2-carboxamide showed the highest anti-cancer activity at a concentration of 20 μg/mL against hepatocellular carcinoma, with a cell viability of 33.29%. All compounds showed significant anti-cancer activity against HepG2, Huh-7, and MCF-7, while indazole and 2,4-dinitrophenyl containing carboxamide derivatives were found to be less potent against all tested cell lines. Results were compared with the standard drug doxorubicin. Carboxamide derivatives possessing 2,4-dinitrophenyl showed significant inhibition against all bacterial and fungal strains with inhibition zones (I.Z) in the range of 9–17 and MICs were found to be 150.7–295 μg/mL. All carboxamide derivatives showed significant anti-fungal activity against all tested fungal strains. Gentamicin was used as the standard drug. The results showed that carbamothioyl-furan-2-carboxamide derivatives could be a potential source of anti-cancer and anti-microbial agents. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents: Design, Synthesis and Activity)
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26 pages, 5963 KiB  
Article
Antimicrobial Efficiency of Chitosan and Its Methylated Derivative against Lentilactobacillus parabuchneri Biofilms
by Diellza Bajrami, Stephan Fischer, Holger Barth, Syed Imdadul Hossain, Nicola Cioffi and Boris Mizaikoff
Molecules 2022, 27(24), 8647; https://doi.org/10.3390/molecules27248647 - 07 Dec 2022
Cited by 5 | Viewed by 2126
Abstract
Antimicrobial materials are considered potential alternatives to prevent the development of biofilm-associated contaminations. Concerns regarding synthetic preservatives necessitate the development of innovative and safe natural antimicrobials. In the present study, we discuss the in situ infrared attenuated total reflection spectroscopy (IR-ATR) investigations of [...] Read more.
Antimicrobial materials are considered potential alternatives to prevent the development of biofilm-associated contaminations. Concerns regarding synthetic preservatives necessitate the development of innovative and safe natural antimicrobials. In the present study, we discuss the in situ infrared attenuated total reflection spectroscopy (IR-ATR) investigations of the selective antimicrobial efficiency of chitosan in controlling the growth of Lentilactobacillus parabuchneri biofilms. The protonated charges of chitosan were additionally amplified by structural modification via methylation, yielding quaternized derivative TMC (i.e., N, N, N-trimethyl chitosan). To evaluate antimicrobial effectiveness against L. parab. biofilms, IR-ATR spectroscopy provided information on molecular mechanisms and insights into chemical changes during real-time biofilm inhibition studies. The integrated fiberoptic oxygen microsensors enabled monitoring oxygen (O2) concentration gradients within biofilms, thereby confirming the metabolic oxygen depletion dropping from 4.5 to 0.7 mg L−1. IR studies revealed strong electrostatic interactions between chitosan/its water-soluble derivative and bacteria, indicating that a few hours were sufficient to affect biofilm disruption. The significant decrease in the IR bands is related to the characteristic spectral information of amide I, II, III, nucleic acid, and extracellular polymeric matrix (EPS) produced by L. parabuchneri biofilms. Cell clusters of biofilms, microcolonies, and destabilization of the EPS matrix after the addition of biopolymers were visualized using optical microscopy. In addition, scanning electron microscopy (SEM) of biofilms grown on polystyrene and stainless-steel surfaces was used to examine morphological changes, indicating the disintegration of the biofilm matrix into individual cells. Quantification of the total biofilm formation correlated with the CV assay results, indicating cell death and lysis. The electrostatic interactions between chitosan and the bacterial cell wall typically occur between protonated amino groups and negatively charged phospholipids, which promote permeabilization. Biofilm growth inhibition was assessed by a viability assay for a period of 72 h and in the range of low MIC values (varying 0.01–2%). These results support the potential of chitosan and TMC for bacterial growth prevention of the foodborne contaminant L. parabuchneri in the dairy industry and for further implementation in food packaging. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents: Design, Synthesis and Activity)
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26 pages, 3480 KiB  
Article
Highly Active Small Aminated Quinolinequinones against Drug-Resistant Staphylococcus aureus and Candida albicans
by Hatice Yıldırım, Nilüfer Bayrak, Mahmut Yıldız, Fatıma Nur Yılmaz, Emel Mataracı-Kara, Deepak Shilkar, Venkatesan Jayaprakash and Amaç Fatih TuYuN
Molecules 2022, 27(9), 2923; https://doi.org/10.3390/molecules27092923 - 03 May 2022
Cited by 5 | Viewed by 2107
Abstract
Two subseries of aminated quinolinequinones (AQQs, AQQ1–16) containing electron-withdrawing group (EWG) or electron-donating group (EDG) in aryl amine moiety were successfully synthesized. Antimicrobial activity assessment indicates that some of the AQQs (AQQ8–10 and AQQ12–14) [...] Read more.
Two subseries of aminated quinolinequinones (AQQs, AQQ1–16) containing electron-withdrawing group (EWG) or electron-donating group (EDG) in aryl amine moiety were successfully synthesized. Antimicrobial activity assessment indicates that some of the AQQs (AQQ8–10 and AQQ12–14) with an EDG in aryl amine exhibited strong antibacterial activity against Gram-positive bacterial strains, including Staphylococcus aureus (ATCC® 29213) and Enterococcus faecalis (ATCC® 29212). In contrast, AQQ4 with an EWG in aryl amine displayed excellent antifungal activity against fungi Candida albicans (ATCC® 10231) with a MIC value of 1.22 μg/mL. To explore the mode of action, the selected AQQs (AQQ4 and AQQ9) were further evaluated in vitro to determine their antimicrobial activity against each of 20 clinically obtained resistant strains of Gram-positive bacteria by performing antibiofilm activity assay and time-kill curve assay. In addition, in silico studies were carried out to determine the possible mechanism of action observed in vitro. The data obtained from these experiments suggests that these molecules could be used to target pathogens in different modes of growth, such as planktonic and biofilm. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents: Design, Synthesis and Activity)
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Review

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15 pages, 1482 KiB  
Review
β-Barrel Assembly Machinery (BAM) Complex as Novel Antibacterial Drug Target
by Qian Xu, Min Guo and Feiyuan Yu
Molecules 2023, 28(9), 3758; https://doi.org/10.3390/molecules28093758 - 27 Apr 2023
Cited by 4 | Viewed by 1926
Abstract
The outer membrane of Gram-negative bacteria is closely related to the pathogenicity and drug resistance of bacteria. Outer membrane proteins (OMPs) are a class of proteins with important biological functions on the outer membrane. The β-barrel assembly machinery (BAM) complex plays a key [...] Read more.
The outer membrane of Gram-negative bacteria is closely related to the pathogenicity and drug resistance of bacteria. Outer membrane proteins (OMPs) are a class of proteins with important biological functions on the outer membrane. The β-barrel assembly machinery (BAM) complex plays a key role in OMP biogenesis, which ensures that the OMP is inserted into the outer membrane in a correct folding manner and performs nutrient uptake, antibiotic resistance, cell adhesion, cell signaling, and maintenance of membrane stability and other functions. The BAM complex is highly conserved among Gram-negative bacteria. The abnormality of the BAM complex will lead to the obstruction of OMP folding, affect the function of the outer membrane, and eventually lead to bacterial death. In view of the important role of the BAM complex in OMP biogenesis, the BAM complex has become an attractive target for the development of new antibacterial drugs against Gram-negative bacteria. Here, we summarize the structure and function of the BAM complex and review the latest research progress of antibacterial drugs targeting BAM in order to provide a new perspective for the development of antibiotics. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents: Design, Synthesis and Activity)
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28 pages, 5206 KiB  
Review
The Multifaceted MEP Pathway: Towards New Therapeutic Perspectives
by Alizée Allamand, Teresa Piechowiak, Didier Lièvremont, Michel Rohmer and Catherine Grosdemange-Billiard
Molecules 2023, 28(3), 1403; https://doi.org/10.3390/molecules28031403 - 01 Feb 2023
Cited by 3 | Viewed by 2597
Abstract
Isoprenoids, a diverse class of natural products, are present in all living organisms. Their two universal building blocks are synthesized via two independent pathways: the mevalonate pathway and the 2-C-methyl-ᴅ-erythritol 4-phosphate (MEP) pathway. The presence of the latter in pathogenic bacteria [...] Read more.
Isoprenoids, a diverse class of natural products, are present in all living organisms. Their two universal building blocks are synthesized via two independent pathways: the mevalonate pathway and the 2-C-methyl-ᴅ-erythritol 4-phosphate (MEP) pathway. The presence of the latter in pathogenic bacteria and its absence in humans make all its enzymes suitable targets for the development of novel antibacterial drugs. (E)-4-Hydroxy-3-methyl-but-2-enyl diphosphate (HMBPP), the last intermediate of this pathway, is a natural ligand for the human Vγ9Vδ2 T cells and the most potent natural phosphoantigen known to date. Moreover, 5-hydroxypentane-2,3-dione, a metabolite produced by Escherichia coli 1-deoxy-ᴅ-xylulose 5-phosphate synthase (DXS), the first enzyme of the MEP pathway, structurally resembles (S)-4,5-dihydroxy-2,3-pentanedione, a signal molecule implied in bacterial cell communication. In this review, we shed light on the diversity of potential uses of the MEP pathway in antibacterial therapies, starting with an overview of the antibacterials developed for each of its enzymes. Then, we provide insight into HMBPP, its synthetic analogs, and their prodrugs. Finally, we discuss the potential contribution of the MEP pathway to quorum sensing mechanisms. The MEP pathway, providing simultaneously antibacterial drug targets and potent immunostimulants, coupled with its potential role in bacterial cell–cell communication, opens new therapeutic perspectives. Full article
(This article belongs to the Special Issue Novel Antimicrobial Agents: Design, Synthesis and Activity)
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