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Antibiotics
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Recent Advances in Antimicrobial Drug Discovery
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Recent Advances in Antimicrobial Drug Discovery

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

Deadline for manuscript submissions: closed (10 June 2023) | Viewed by 15248

Special Issue Editor

Dr. Melissa M. Cadelis

E-Mail Website
Guest Editor
School of Medical Sciences, University of Auckland, Auckland 1142, New Zealand
Interests: natural product; medicinal chemistry; organic chemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Antibiotics have been the cornerstone of modern medicine saving lives by virtue of being able to cure infectious diseases and to prevent infections in those that are immune compromised. Their intense use has led to a surging increase in the incidence of antibiotic-resistant bacteria resulting in a desperate need for antibiotics with new mechanisms of action. Natural products, originating from marine, plant and fungal origins, are rich sources of bioactive compounds with diverse structures and functional groups and have given society some of the largest medical breakthroughs in our time. In this Special Issue we welcome the submission of publications of research and review articles on the discovery of natural products or synthetic derivatives with antibacterial activities, and studies clarifying their mechanisms and modes of action.

Dr. Melissa M. Cadelis
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. 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.

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Published Papers (6 papers)

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Research

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15 pages, 1026 KiB  
Article
Synthesis, Antibacterial and Antiribosomal Activity of the 3C-Aminoalkyl Modification in the Ribofuranosyl Ring of Apralogs (5-O-Ribofuranosyl Apramycins)
by Dmitrijs Lubriks, Klara Haldimann, Sven N. Hobbie, Andrea Vasella, Edgars Suna and David Crich
Antibiotics 2023, 12(1), 25; https://doi.org/10.3390/antibiotics12010025 - 24 Dec 2022
Cited by 2 | Viewed by 1525
Abstract
The synthesis and antiribosomal and antibacterial activity of both anomers of a novel apralog, 5-O-(5-amino-3-C-dimethylaminopropyl-D-ribofuranosyl)apramycin, are reported. Both anomers show excellent activity for the inhibition of bacterial ribosomes and that of MRSA and various wild-type Gram negative pathogens. The [...] Read more.
The synthesis and antiribosomal and antibacterial activity of both anomers of a novel apralog, 5-O-(5-amino-3-C-dimethylaminopropyl-D-ribofuranosyl)apramycin, are reported. Both anomers show excellent activity for the inhibition of bacterial ribosomes and that of MRSA and various wild-type Gram negative pathogens. The new compounds retain activity in the presence of the aminoglycoside phosphoryltransferase aminoglycoside modifying enzymes that act on the primary hydroxy group of typical 4,5-(2-deoxystreptamine)-type aminoglycoside and related apramycin derivatives. Unexpectedly, the two anomers have comparable activity both for the inhibition of bacterial ribosomes and of the various bacterial strains tested. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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10 pages, 1180 KiB  
Article
Screening and Molecular Docking of Bioactive Metabolites of the Red Sea Sponge Callyspongia siphonella as Potential Antimicrobial Agents
by Arafa Musa, Mohamed A. Abdelgawad, Mohamed E. Shaker, Ahmed H. El-Ghorab, Della Grace Thomas Parambi, Ahmed A. Hamed, Ahmed M. Sayed, Hossam M. Hassan and Mahmoud A. Aboseada
Antibiotics 2022, 11(12), 1682; https://doi.org/10.3390/antibiotics11121682 - 23 Nov 2022
Cited by 2 | Viewed by 1466
Abstract
Marine sponges create a wide range of bioactive secondary metabolites, as documented throughout the year. Several bioactive secondary metabolites were isolated from different members of Callyspongia siphonella species. This study aimed for isolation and structural elucidation of major metabolites in order to investigate [...] Read more.
Marine sponges create a wide range of bioactive secondary metabolites, as documented throughout the year. Several bioactive secondary metabolites were isolated from different members of Callyspongia siphonella species. This study aimed for isolation and structural elucidation of major metabolites in order to investigate their diverse bioactivities such as antimicrobial and anti-biofilm activities. Afterwards, a molecular docking study was conducted, searching for the possible mechanistic pathway of the most bioactive metabolites. Extraction, fractionation, and metabolomics analysis of different fractions was performed in order to obtain complete chemical profile. Moreover, in vitro assessment of different bioactivities was performed, using recent techniques. Additionally, purification, structural elucidation of high features using recent chromatographic and spectroscopic techniques was established. Finally, AutoDock Vina software was used for the Pharmacophore-based docking-based analysis. As a result, DCM (dichloromethane) fraction exerted the best antibacterial activity using disc diffusion method; particularly against S. aureus with an inhibition zone of 6.6 mm. Compound 11 displayed a considerable activity against both MRSA (Methicillin-resistant Staphyllococcus aureus) and Staphyllococcus aureus with inhibition ratios of 50.37 and 60.90%, respectively. Concerning anti-biofilm activity, compounds 1 and 2 displayed powerful activity with inhibition ratios ranging from 39.37% to 70.98%. Pharmacophore-based docking-based analysis suggested elongation factor G (EF-G) to be a probable target for compound 11 (siphonellinol C) that showed the best in vitro antibacterial activity, offering unexplored potential for new drugs and treatment candidates. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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46 pages, 2891 KiB  
Article
Discovery and Preliminary Structure-Activity Investigation of 3-Substituted-1H-imidazol-5-yl-1H-indoles with In Vitro Activity towards Methicillin-Resistant Staphylococcus aureus
by Steven A. Li, Rebecca J. Zheng, Kenneth Sue, Marie-Lise Bourguet-Kondracki, Azza Troudi, Jean Michel Brunel, Brent R. Copp and Melissa M. Cadelis
Antibiotics 2022, 11(10), 1450; https://doi.org/10.3390/antibiotics11101450 - 21 Oct 2022
Viewed by 1264
Abstract
Antibiotics have been the cornerstone of modern medicine saving lives by virtue of being able to cure infectious diseases and to prevent infections in those who are immune compromised. Their intense use has led to a surging increase in the incidence of antibiotic-resistant [...] Read more.
Antibiotics have been the cornerstone of modern medicine saving lives by virtue of being able to cure infectious diseases and to prevent infections in those who are immune compromised. Their intense use has led to a surging increase in the incidence of antibiotic-resistant bacteria resulting in a desperate need for antibiotics with new mechanisms of action. As part of our search for new antimicrobials we have screened an in-house library of compounds and identified two 3-substituted-1H-imidazol-5-yl-1H-indoles as weak growth inhibitors (MIC 16 µg/mL) against methicillin-resistant Staphylococcus aureus (MRSA). An extensive library of analogues was prepared using the Van Leusen three-component reaction, biological evaluation of which led to the identification of two analogues (26 and 32) with favorable anti-MRSA activity (MIC ≤ 0.25 µg/mL) which also lacked cytotoxic or hemolytic properties. The screening campaign also identified two derivatives, a phenethyl-indole-imidazole 57 and a 5-phenyl-1H-imidazole 111 that were non-toxic selective antifungals towards Cryptococcus neoformans. These results have identified 3-substituted-1H-imidazol-5-yl-1H-indoles and 5-phenyl-1H-imidazoles as new structural scaffolds for further investigation as anti-MRSA and anti-C. neoformans agents, respectively. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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18 pages, 1568 KiB  
Article
Phytochemical Composition, Antioxidant and Antifungal Activity of Thymus capitatus, a Medicinal Plant Collected from Northern Morocco
by Amina Benoutman, El Hadi Erbiai, Fatima Zahra Edderdaki, El Khalil Cherif, Rabah Saidi, Zouhaire Lamrani, Manuela Pintado, Eugénia Pinto, Joaquim C. G. Esteves da Silva and Abdelfettah Maouni
Antibiotics 2022, 11(5), 681; https://doi.org/10.3390/antibiotics11050681 - 18 May 2022
Cited by 14 | Viewed by 2622
Abstract
Thymus capitatus is a Mediterranean endemic plant commonly known as “Zaïtra” in northern Morocco. As T. capitatus is widely used in traditional medicine and food, this present work aims to investigate the chemical compositions and biological activities of the T. capitatus leaves essential [...] Read more.
Thymus capitatus is a Mediterranean endemic plant commonly known as “Zaïtra” in northern Morocco. As T. capitatus is widely used in traditional medicine and food, this present work aims to investigate the chemical compositions and biological activities of the T. capitatus leaves essential oil (TcLEO), acetonic (TcLAE), and methanolic extract (TcLME). The spectrophotometric determination demonstrated that T. capitatus is a natural source rich in phenolic contents (TPC) and flavonoid contents (TFC) and that TcLME revealed the highest TPC and TFC than TcLAE and TcLEO. The LC-MS analysis of phenolic compounds showed that paraben acid was predominant in both TcLME and TcLAE, followed by cinnamic acid and p-hydroxybenzoic acid. GC-MS analysis of the TcLEO revealed the presence of a total of 10 compounds, which were predominated by carvacrol. The antioxidant activity by ORAC was observed to be significantly higher in TcLEO and TcLAE than in TcLME. All samples used to assess DNA degradation effectively prevented DNA oxidation and, at the same time, had a prooxidant effect. The genotoxicity test showed that the T. capitatus were devoid of any mutagenic activity. Concerning antifungal activity, all samples were able to inhibit the growth of all microorganisms tested at low concentrations. TcLAE showed higher activity than TcLME, and in general, dermatophytes were more susceptible, being Microsporum canis the most sensitive one. Overall, the results obtained from this study confirm the wide uses of T. capitatus. Furthermore, the finding results suggest that the T. capitatus essential oil and extracts can be highly useful for pharmaceutical industries. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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14 pages, 4172 KiB  
Article
Effects of Curcumin and Tetracycline Gel on Experimental Induced Periodontitis as an Anti-Inflammatory, Osteogenesis Promoter and Enhanced Bone Density through Altered Iron Levels: Histopathological Study
by Chenar Anwar Mohammad, Khadeeja Mohammed Ali, Rafal AbdulRazaq Al-Rawi and Sarhang Sarwat Gul
Antibiotics 2022, 11(4), 521; https://doi.org/10.3390/antibiotics11040521 - 13 Apr 2022
Cited by 4 | Viewed by 2069
Abstract
Adjunctive use of antimicrobials with scaling and root planing (SRP) is necessary to better eradicate dental biofilm. Tetracycline (T) is the most commonly used antimicrobial; however, it has limitations. This study evaluates the effect of curcumin (CU) as adjunct to SRP on inflammatory [...] Read more.
Adjunctive use of antimicrobials with scaling and root planing (SRP) is necessary to better eradicate dental biofilm. Tetracycline (T) is the most commonly used antimicrobial; however, it has limitations. This study evaluates the effect of curcumin (CU) as adjunct to SRP on inflammatory markers, collagen fiber deposition, and altered iron level. A total of 32 Wistar rats were divided into five groups: no experimental periodontitis (healthy control), experimental periodontitis (EPD), EPD treated with SRP alone (SRP), EPD treated with SRP+T (SRP+T), and EPD treated with SRP+CU (SRP+CU). After 2 and 4 weeks of treatment, tissue samples were assessed by hematoxylin and eosin, and special stains (Perls’ stain and Masson’s Trichrome) for counting of inflammatory cells, angiogenesis, collagen fibers, and iron deposition. Significant reductions in inflammatory cells infiltration and alveolar bone resorption with angiogenesis and collagen fibers deposition were detected after 2 and 4 weeks in both SRP+T and SRP+CU groups. SRP+CU resulted in a significant reduction in osteoclast numbers (week 2) and iron deposition (week 4) in bone trabeculae as compared to SRP and SRP+T groups. The adjunctive use of CU showed comparable results to T in the reduction in inflammation and bone resorption. Furthermore, CU has potential osteogenesis and healing effects. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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18 pages, 711 KiB  
Systematic Review
Antibacterial Properties of Eucalyptus globulus Essential Oil against MRSA: A Systematic Review
by Shakthi Elangovan and Poonam Mudgil
Antibiotics 2023, 12(3), 474; https://doi.org/10.3390/antibiotics12030474 - 27 Feb 2023
Cited by 12 | Viewed by 5299
Abstract
Antimicrobial resistance is a huge threat against the public health sphere and is a major cause of global mortality and morbidity. Antibiotic misuse and overuse have led to the development of many resistant bacterial strains. One particular bacterium of concern is methicillin-resistant Staphylococcus [...] Read more.
Antimicrobial resistance is a huge threat against the public health sphere and is a major cause of global mortality and morbidity. Antibiotic misuse and overuse have led to the development of many resistant bacterial strains. One particular bacterium of concern is methicillin-resistant Staphylococcus aureus (MRSA), which is the most common resistant bacteria in humans. Antibiotic development has been unable to keep up with the rapid evolution of antibiotic-resistant organisms, and there is an urgent need to identify alternative agents to combat this problem. The purpose of this systematic review is to explore the literature on the antibacterial properties of Eucalyptus globulus essential oil against MRSA. The articles used in this review were obtained through a systematic search of the literature across four databases, with the timeline being between 2002 and 2022. Twenty studies were included in this review, which used various methods to investigate the antibacterial properties of E. globulus essential oil, alone or in combination with other agents, against MRSA. The findings suggest that E. globulus essential oil has antibacterial properties against MRSA, which can be enhanced when used in combination with other agents, such as other essential oils and antibiotics. Full article
(This article belongs to the Special Issue Recent Advances in Antimicrobial Drug Discovery)
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