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Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing

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

Deadline for manuscript submissions: closed (30 November 2020) | Viewed by 32928

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Special Issue Editors

Dr. Ioana Matei

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Guest Editor

Department of Microbiology (Veterinary Medicine), University of Agricultural Sciences and Veterinary Medicine, Cluj-Napoca, Romania
Interests: natural antimicrobial molecules; chemically synthetized and/or modified antimicrobial molecules; antimicrobial potential testing; natural products testing; antimicrobial resistance
Special Issues, Collections and Topics in MDPI journals

Dr. Gabriel Marc

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Guest Editor

Department of Pharmaceutical Chemistry, Iuliu Hațieganu University of Medicine and Pharmacy, 41 Victor Babeș Street, RO-400012 Cluj-Napoca, Romania
Interests: chemically synthetized and/or modified antimicrobial molecules; antimicrobial potential testing; antimicrobial resistance; molecular docking; molecular descriptors
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The emergence of antimicrobial-resistant (AMR) bacteria is becoming a topic of critical importance in both human and veterinary medicine. There is a recent concern related to the possibility of AMR transmission in both commensal and zoonotic bacteria, which may explain the increasing prevalence of AMR bacteria. The social impact is estimated by ECDC at 25,000 deaths per year in the EU alone and 700,000 deaths per year globally which are caused by AMR bacteria. In this context, the development of new therapeutic strategies is needed. Alongside AMR prevention and control, the AMR combat plan includes research, development, and innovation within the following lines: (i) the discovery of new antibiotics; (ii) the design and synthesis of conventional antibiotic derivates in order to decrease the AMR; (iii) to investigate the antimicrobial potential of alternative compounds in order to replace or support conventional antibiotic therapy.

In this context, this Special Issue aims to gather the latest data regarding the synthesis and development of new antibiotic drugs and the identification of new compounds with antibiotic potential. Therefore, we invite authors to submit original research or reviews covering all aspects of this theme.

Dr. Ioana Matei
Dr. Gabriel Marc
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

antibiotics synthesis
antimicrobial potential
novel anti-microbials

Published Papers (7 papers)

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Research

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17 pages, 6383 KiB

Open AccessArticle

A Cationic Porphyrin, ZnPor, Disassembles Pseudomonas aeruginosa Biofilm Matrix, Kills Cells Directly, and Enhances Antibiotic Activity of Tobramycin

by Neha Patel, Shawn Swavey and Jayne Robinson

Antibiotics 2020, 9(12), 875; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9120875 - 06 Dec 2020

Cited by 8 | Viewed by 2665

Abstract

One of the greatest threats to human health is the rise in antibiotic-resistant bacterial infections. Pseudomonas aeruginosa (PsA) is an “opportunistic” pathogen known to cause life-threatening infections in immunocompromised individuals and is the most common pathogen in adults with cystic fibrosis (CF). We report here a cationic zinc (II) porphyrin, ZnPor, that effectively kills planktonic and biofilm-associated cells of PsA. In standard tests against 16–18 h-old biofilms, concentrations as low as 16 µg/mL resulted in the extensive disruption and detachment of the matrix. The pre-treatment of biofilms for 30 min with ZnPor at minimum inhibitory concentration (MIC) levels (4 µg/mL) substantially enhanced the ability of tobramycin (Tobra) to kill biofilm-associated cells. We demonstrate the rapid uptake and accumulation of ZnPor in planktonic cells even in dedicated heme-uptake system mutants (ΔPhu, ΔHas, and the double mutant). Furthermore, uptake was unaffected by the ionophore carbonyl cyanide m-chlorophenyl hydrazine (CCCP). Cells pre-exposed to ZnPor took up the cell-impermeant dye SYTOX^TM Green in a concentration-dependent manner. The accumulation of ZnPor did not result in cell lysis, nor did the cells develop resistance. Taken together, these properties make ZnPor a promising candidate for treating multi-drug-resistant infections, including persistent, antibiotic-resistant biofilms. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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21 pages, 15918 KiB

Open AccessArticle

Mutually Isomeric 2- and 4-(3-Nitro-1,2,4-triazol-1-yl)pyrimidines Inspired by an Antimycobacterial Screening Hit: Synthesis and Biological Activity against the ESKAPE Panel of Pathogens

by Sergey Chuprun, Dmitry Dar’in, Elizaveta Rogacheva, Liudmila Kraeva, Oleg Levin, Olga Manicheva, Marine Dogonadze, Tatiana Vinogradova, Olga Bakulina and Mikhail Krasavin

Antibiotics 2020, 9(10), 666; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9100666 - 01 Oct 2020

Cited by 5 | Viewed by 3892

Abstract

Starting from the structure of antimycobacterial screening hit OTB-021 which was devoid of activity against ESKAPE pathogens, we designed, synthesized and tested two mutually isomeric series of novel simplified analogs, 2- and 4-(3-nitro-1,2,4-triazol-1-yl)pyrimidines, bearing various amino side chains. These compounds demonstrated a reverse bioactivity profile being inactive against M. tuberculosis while inhibiting the growth of all ESKAPE pathogens (with variable potency patterns) except for Gram-negative P. aeruginosa. Reduction potentials (E_1/2, V) measured for selected compounds by cyclic voltammetry were tightly grouped in the −1.3–−1.1 V range for a reversible single-electron reduction. No apparent correlation between the E_1/2 values and the ESKAPE minimum inhibitory concentrations was established, suggesting possible significance of other factors, besides the compounds’ reduction potential, which determine the observed antibacterial activity. Generally, more negative E_1/2 values were displayed by 2-(3-nitro-1,2,4-triazol-1-yl)pyrimidines, which is in line with the frequently observed activity loss on moving the 3-nitro-1,2,4-triazol-1-yl moiety from position 4 to position 2 of the pyrimidine nucleus. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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18 pages, 5373 KiB

Open AccessArticle

Endophytic Streptomyces laurentii Mediated Green Synthesis of Ag-NPs with Antibacterial and Anticancer Properties for Developing Functional Textile Fabric Properties

by Ahmed M. Eid, Amr Fouda, Gniewko Niedbała, Saad El-Din Hassan, Salem S. Salem, Abdullah M. Abdo, Helal F. Hetta and Tharwat I. Shaheen

Antibiotics 2020, 9(10), 641; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9100641 - 24 Sep 2020

Cited by 121 | Viewed by 5833

Abstract

Improvement of the medical textile industry has received more attention recently, especially with widespread of microbial and viral infections. Medical textiles with new properties, such as bacterial pathogens self-cleaning, have been explored with nanotechnology. In this study, an endophytic actinomycetes strain of Streptomyces laurentii R-1 was isolated from the roots of the medicinal plant Achillea fragrantissima. This is used as a catalyst for the mediated biosynthesis of silver nanoparticles (Ag-NPs) for applications in the textile industry. The biosynthesized Ag-NPs were characterized using UV-vis spectroscopy, Fourier transform infrared (FT-IR), transmission electron microscopy (TEM), and X-ray Diffraction (XRD), which confirmed the successful formation of crystalline, spherical metal nanoparticles. The biosynthesized Ag-NPs exhibited broad-spectrum antibacterial activity. Our data elucidated that the biosynthesized Ag-NPs had a highly cytotoxic effect against the cancerous caco-2 cell line. The selected safe dose of Ag-NPs for loading on cotton fabrics was 100 ppm, regarding their antibacterial activity and safe cytotoxic efficacy. Interestingly, scanning electron microscope connected with energy dispersive X-ray spectroscopy (SEM-EDX) of loaded cotton fabrics demonstrated the smooth distribution of Ag-NPs on treated fabrics. The obtained results highlighted the broad-spectrum activity of nano-finished fabrics against pathogenic bacteria, even after 5 and 10 washing cycles. This study contributes a suitable guide for the performance of green synthesized NPs for utilization in different biotechnological sectors. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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13 pages, 1837 KiB

Open AccessArticle

Efficacy and Gut Dysbiosis of Gentamicin-Intercalated Smectite as a New Therapeutic Agent against Helicobacter pylori in a Mouse Model

by Su Jin Jeong, Kyoung Hwa Lee, Jie-Hyun Kim, Soon Young Park and Young Goo Song

Antibiotics 2020, 9(8), 502; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9080502 - 10 Aug 2020

Cited by 6 | Viewed by 3395

Abstract

Helicobacter pylori eradication rate with conventional standard therapy is decreasing owing to antibiotic resistance, necessitating novel antibacterial strategies against H. pylori. We evaluated the efficacy of a gentamicin-intercalated smectite hybrid (S-GM)-based treatment and analyzed fecal microbiome composition in H. pylori-infected mice. To evaluate anti-H. pylori efficacy, mice were divided into eight groups, and H. pylori eradication was assessed by a Campylobacter-like organism (CLO) test and PCR assay of H. pylori in gastric mucosa. One week after H. pylori eradication, pro-inflammatory cytokine levels and atrophic changes in gastric mucosa were examined. Stool specimens were collected and analyzed for microbiome changes. The S-GM-based triple regimen decreased bacterial burden in vivo, compared with that in untreated mice or mice treated with other regimens. The therapeutic reactions in the CLO test from gastric mucosa were both 90% in the standard triple therapy and S-GM therapy group, respectively. Those of H. pylori PCR in mouse gastric mucosa were significantly lower in standard triple therapy and S-GM therapy groups than in the non-treatment group. Toxicity test results showed that S-GM therapy reduced IL-8 level and atrophic changes in gastric mucosa. Stool microbiome analysis revealed that compared with mice treated with the standard triple therapy, mice treated with the S-GM therapy showed microbiome diversity and abundant microorganisms at the phylum level. Our results suggested that S-GM is a promising and effective therapeutic agent against H. pylori infection. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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13 pages, 5366 KiB

Open AccessArticle

Crystallography, in Silico Studies, and In Vitro Antifungal Studies of 2,4,5 Trisubstituted 1,2,3-Triazole Analogues

by Katharigatta N. Venugopala, Mohammed A. Khedr, Yarabahally R. Girish, Subhrajyoti Bhandary, Deepak Chopra, Mohamed A. Morsy, Bandar E. Aldhubiab, Pran Kishore Deb, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Rashmi V, Mahmoud Kandeel, Sabah H. Akrawi, Madhusudana Reddy M B, Sheena Shashikanth, Osama I. Alwassil and Viresh Mohanlall

Antibiotics 2020, 9(6), 350; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9060350 - 20 Jun 2020

Cited by 13 | Viewed by 3432

Abstract

A series of 2,4,5 trisubstituted-1,2,3-triazole analogues have been screened for their antifungal activity against five fungal strains, Candida parapsilosis, Candida albicans, Candida tropicalis, Aspergillus niger, and Trichophyton rubrum, via a 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide (MTT) microdilution assay. Compounds GKV10, GKV11, and GKV15 emerged as promising antifungal agents against all the fungal strains used in the current study. One of the highly active antifungal compounds, GKV10, was selected for a single-crystal X-ray diffraction analysis to unequivocally establish its molecular structure, conformation, and to understand the presence of different intermolecular interactions in its crystal lattice. A cooperative synergy of the C-H···O, C-H···N, C-H···S, C-H···π, and π···π intermolecular interactions was present in the crystal structure, which contributed towards the overall stabilization of the lattice. A molecular docking study was conducted for all the test compounds against Candida albicans lanosterol-14α-demethylase (pdb = 5 tzl). The binding stability of the highly promising antifungal test compound, GKV15, from the series was then evaluated by molecular dynamics studies. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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18 pages, 4953 KiB

Open AccessArticle

Identification and Testing of Antidermatophytic Oxaborole-6-Benzene Sulphonamide Derivative (OXBS) from Streptomyces atrovirens KM192347 Isolated from Soil

by Seham Abdel-Shafi, Abdul-Raouf Al-Mohammadi, Taghreed N. Almanaa, Ahmed H. Moustafa, Tamer M. M. Saad, Abdel-Rahman Ghonemey, Immacolata Anacarso, Gamal Enan and Nashwa El-Gazzar

Antibiotics 2020, 9(4), 176; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics9040176 - 13 Apr 2020

Cited by 18 | Viewed by 3085

Abstract

There is a need to continue research to find out other anti-dermatophytic agents to inhibit causal pathogenic skin diseases including many types of tinea. We undertook the production, purification, and identification of an anti-dermatophytic substance by Streptomyces atrovirens. Out of 103 streptomycete isolates tested, only 20 of them showed antidermatophytic activity with variable degrees against Trichophyton tonsurans CCASU 56400 (T. tonsurans), Microsporum canis CCASU 56402 (M. canis), and Trichophyton mentagrophytes CCASU 56404 (T. mentagrophytes). The most potent isolate, S₁₀Q₆, was identified based on the tests conducted that identified morphological and physiological characteristics and using 16S rRNA gene sequencing. The isolate was found to be closely correlated to previously described species Streptomyces atrovirens; it was designated Streptomyces atrovirens KM192347 (S. atrovirens). Maximum antifungal activity of the strain KM192347 was obtained in modified starch nitrate medium (MSNM) adjusted initially at pH 7.0 and incubated at 30 °C in shaken cultures (150 rpm) for seven days. The antifungal compound was purified by using two steps protocol including solvent extraction and column chromatography. The MIC of it was 20 µg/mL against the dermatophyte cultures tested. According to the data obtained from instrumental analysis and surveying the novel antibiotics database, the antidermatophytic substance produced by the strain KM192347 was characterized as an oxaborole-6-benzene sulphonamide derivative and designated oxaborole-6-benzene sulphonamide (OXBS) with the chemical formula C₁₃H₁₂ BNO₄S. The crude OXBS didn’t show any toxicity on living cells. Finally, the results obtained herein described another anti-dermatophytic substance named an OXBS derivative. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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Review

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15 pages, 1226 KiB

Open AccessReview

From Evidence to Clinical Guidelines in Antibiotic Treatment in Acute Otitis Media in Children

by Elena Lia Spoială, Gabriela Dumitrita Stanciu, Veronica Bild, Daniela Carmen Ababei and Cristina Gavrilovici

Antibiotics 2021, 10(1), 52; https://0-doi-org.brum.beds.ac.uk/10.3390/antibiotics10010052 - 06 Jan 2021

Cited by 9 | Viewed by 9782

Abstract

Acute otitis media (AOM) in children represents a public health concern, being one of the leading causes of health care visits and antibiotic prescriptions worldwide. The overall aim of this paper is to unravel the major current insights into the antibiotic treatment of AOM in children. Our approach is three-fold: 1. a preclinical evaluation of antibiotics in animal models of AOM stressing on the advantages of different species when testing for different schemes of antibiotics; 2. an overview on the new antimicrobial agents whose efficacy has been demonstrated in refractory cases of AOM in children; and 3. an analysis of the different guidelines stressing on the differences and similarities between the various schemes of antibiotic treatment. The preferred therapeutic agents remain amoxicillin and the amoxicillin-clavulanate combination for AOM caused by Streptococcus pneumoniae, whereas oral cephalosporin is preferred in AOM due to Moraxella catarrhalis and Haemophilus influenzae. As for the second and third line antimicrobial treatments, there is a wide variety of suggested antibiotic classes with variations in duration and posology. The decision to prescribe antimicrobial treatment as a first-line choice is based on the severity of the symptoms in 16 of the guidelines included in this review. Full article

(This article belongs to the Special Issue Antibiotic Drug Synthesis and New Antimicrobial Compounds Identification and Testing)

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