Discovery of a novel class of small-molecule antibacterial agents against Staphylococcus aureus

2021 ◽  
Author(s):  
David Kreutzer ◽  
Robin Gehrmann ◽  
Annámaria Kincses ◽  
Nikoletta Szemerédi ◽  
Gabriella Spengler ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Small Molecule ◽  
Antibacterial Agents ◽  
Antibacterial Effects ◽  
Molecular Scaffold ◽  
Antibacterial Compounds ◽  
Aromatic Residue ◽  
Lead Compounds ◽  
Step Procedure

Background: With constantly increasing resistance against the known antibiotics, the search for novel antibacterial compounds is a challenge. The number of synthetic antibacterial agents is limited. Materials & methods: We discovered novel small-molecule antibacterial agents that are accessible via a simple two-step procedure. The evaluation against Staphylococcus aureus showed antibacterial effects depending on the substituent positioning at the residues of the molecular scaffold. Additionally, we investigated the potential of the compounds to increase the antibacterial activity of tetracycline. Results: The most effective antibacterial compounds possessed a 3-methoxy function at an aromatic residue. In combination with tetracycline, we found a strong effect for a few compounds in boosting the antibacterial activity, so the first promising lead compounds with dual activities could be identified.

scholarly journals Novel Small-Molecule Hybrid-Antibacterial Agents against S. aureus and MRSA Strains

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 61
Author(s):  
Robin Gehrmann ◽  
Tobias Hertlein ◽  
Elisa Hopke ◽  
Knut Ohlsen ◽  
Michael Lalk ◽  
...  
Keyword(s):  
Small Molecule ◽  
Antibacterial Agents ◽  
One Pot ◽  
Antibacterial Compounds ◽  
Lead Compounds ◽  
Mrsa Strains ◽  
Novel Structures

Ongoing resistance developments against antibiotics that also affect last-resort antibiotics require novel antibacterial compounds. Strategies to discover such novel structures have been dimerization or hybridization of known antibacterial agents. We found novel antibacterial agents by dimerization of indols and hybridization with carbazoles. They were obtained in a simple one-pot reaction as bisindole tetrahydrocarbazoles. Further oxidation led to bisindole carbazoles with varied substitutions of both the indole and the carbazole scaffold. Both the tetrahydrocarbazoles and the carbazoles have been evaluated in various S. aureus strains, including MRSA strains. Those 5-cyano substituted derivatives showed best activities as determined by MIC values. The tetrahydrocarbazoles partly exceed the activity of the carbazole compounds and thus the activity of the used standard antibiotics. Thus, promising lead compounds could be identified for further studies.

scholarly journals Phosphonopeptides Revisited, in an Era of Increasing Antimicrobial Resistance

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1445 ◽  
Author(s):  
Emma C.L. Marrs ◽  
Linda Varadi ◽  
Alexandre F. Bedernjak ◽  
Kathryn M. Day ◽  
Mark Gray ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Resistance ◽  
Enterococcus Faecalis ◽  
Antibacterial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Peptide Mimetics ◽  
Antibacterial Resistance ◽  
Bacterial Isolates ◽  
New Agents ◽  
Antibacterial Compounds

Given the increase in resistance to antibacterial agents, there is an urgent need for the development of new agents with novel modes of action. As an interim solution, it is also prudent to reinvestigate old or abandoned antibacterial compounds to assess their efficacy in the context of widespread resistance to conventional agents. In the 1970s, much work was performed on the development of peptide mimetics, exemplified by the phosphonopeptide, alafosfalin. We investigated the activity of alafosfalin, di-alanyl fosfalin and β-chloro-L-alanyl-β-chloro-L-alanine against 297 bacterial isolates, including carbapenemase-producing Enterobacterales (CPE) (n = 128), methicillin-resistant Staphylococcus aureus (MRSA) (n = 37) and glycopeptide-resistant enterococci (GRE) (n = 43). The interaction of alafosfalin with meropenem was also examined against 20 isolates of CPE. The MIC50 and MIC90 of alafosfalin for CPE were 1 mg/L and 4 mg/L, respectively and alafosfalin acted synergistically when combined with meropenem against 16 of 20 isolates of CPE. Di-alanyl fosfalin showed potent activity against glycopeptide-resistant isolates of Enterococcus faecalis (MIC90; 0.5 mg/L) and Enterococcus faecium (MIC90; 2 mg/L). Alafosfalin was only moderately active against MRSA (MIC90; 8 mg/L), whereas β-chloro-L-alanyl-β-chloro-L-alanine was slightly more active (MIC90; 4 mg/L). This study shows that phosphonopeptides, including alafosfalin, may have a therapeutic role to play in an era of increasing antibacterial resistance.

scholarly journals Recent advancement in polyphenols as potential antibacterial agents: A comprehensive review

2021 ◽  
Vol 01 ◽  
Author(s):  
Vivek Ahluwalia ◽  
Nusrat Iqbal ◽  
Samsul Alam ◽  
Vinod Kumar ◽  
Lalitesh K. Thakur ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antibiotic Resistance ◽  
Antibacterial Agents ◽  
Dietary Habits ◽  
Antioxidant Properties ◽  
Antibacterial Properties ◽  
Polyphenolic Compounds ◽  
Antibacterial Compounds ◽  
Recent Advancement ◽  
Food Commodities

: New molecules of natural origin with antibacterial properties are urgently required to control the antibiotic resistance. Worldwide, antibiotic resistance is key threats due to non-judicious and incongruous use of antibiotics. Researchers are focusing on identifying molecules from plant biodiversity that could have both antioxidant and antibacterial properties in one molecule. Much importance on natural antibacterial compounds has been given to the polyphenolic compounds from food commodities. The roles of dietary habits in disease prevention have been credited to presence of polyphenols with antioxidant properties. Polyphenols are secondary metabolites with manifold vital roles including antibacterial activity. Numerous mechanisms like bacterial membrane destruction, destruction of virulence factors, inhibition of the enzymes activity and toxins had been reported for antibacterial activity. Also, hydroxyl, alkyl and acetate moiety on aromatic nucleus influences both antioxidant and antibacterial activity. In this review, details are summarized concerning the antibacterial properties of the key polyphenolic compounds with antioxidant properties.

Unveiling the bioactivity of Allium triquetrum L. lipophilic fractions: chemical characterization and in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus

2020 ◽  
Vol 11 (6) ◽  
pp. 5257-5265
Author(s):  
Samia Rabah ◽  
Kahina Kouachi ◽  
Patrícia A. B. Ramos ◽  
Ana Peixoto Gomes ◽  
Adelaide Almeida ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Chemical Characterization ◽  
Value Added ◽  
Lipophilic Compounds ◽  
Methicillin Resistant ◽  
In Vitro Antibacterial Activity

Allium triquetrum L. bulbs, flowers and leaves are proved to be valuable sources of value-added lipophilic compounds, specifically as antibacterial agents against methicillin-resistant Staphylococcus aureus.

Preparation and Antimicrobial Activity of Antibacterial Silver-Loaded Polyphosphazene Microspheres

2021 ◽  
Vol 21 (10) ◽  
pp. 5120-5130
Author(s):  
Hui Long ◽  
Wei-Cong Kuang ◽  
Shi-Liang Wang ◽  
Jing-Xian Zhang ◽  
Lang-Huan Huang ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Thermal Stability ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Silver Nanoparticles ◽  
Antibacterial Activity ◽  
Antibacterial Agents ◽  
Good Thermal Stability ◽  
Polymerization Method

Poly(cyclotriphosphazene-co-4,4’-diaminodiphenyl ether) (PPO) microspheres were prepared via a precipitation polymerization method, using hexachlorocyclotriphosphazene (HCCP) and 4,4’-diaminodiphenyl ether (ODA) as monomers. Silver-loaded PPO (PPOA) microspheres were generated by the in situ loading of silver nanoparticles onto the surface by Ag+ reduction. Our results showed that PPOA microspheres were successfully prepared with a relatively uniform distribution of silver nanoparticles on microsphere surfaces. PPOA microspheres had good thermal stability and excellent antibacterial activity towards Escherichia coli and Staphylococcus aureus. Furthermore, PPOA microspheres exhibited lower cytotoxicity when compared to citrate-modified silver nanoparticles (c-Ag), and good sustained release properties. Our data indicated that polyphosphazene-based PPOA microspheres are promising antibacterial agents in the biological materials field.

scholarly journals Properties of Binuclear Rhodium(II) Complexes and Their Antibacterial Activity

1996 ◽  
Vol 3 (4) ◽  
pp. 185-195 ◽  
Author(s):  
Florian P. Pruchnik ◽  
Małgorzata Bień ◽  
Tadeusz Lachowicz
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nmr Spectroscopy ◽  
Antibacterial Agents ◽  
Structure And Properties ◽  
E Coli ◽  
Nitrogen Ligands ◽  
Low Activity

Binuclear rhodium(II) complexes [Rh2Cl2(μ-OOCR)2(N-N)2], [Rh2(μ-OOCR)2(N-N)2(H2O)2](RCOO)2 and [Rh2Cl2(μ-OOCCH3)(terpy)2](H3O)Cl2.9H2O (R = H, Me, Bun,ph, PhCHOH; N-N = 2,2′-bipyridine (bpy), 1,10-phenanthroline (phen), 2,9-dimethyl-1,10-phenanthroline (dmp) and 6,7-dimethyl-2,3- di(2-pyridyl)quinoxaline (dmpq); terpy 2,2′:6′,2′′-terpyridine) have been synthesized and their structure and properties have been studied by electronic, IR and H1 NMR spectroscopy. Antibacterial activity of these complexes against Staphylococcus aureus and Escherichia coli has been investigated. The most active antibacterial agents against S. aureus were [Rh2(OOCPh)2(phen)2(H2O)2]2+, [Rh2(OOCPh)2(dmpq)2(H2O)2]2+, [Rh2(OOCBu)2(phen)2(H2O)2]2+ and [Rh2-(OOCBu)2(bpy)2(H2O)2]2+ which were considerably more active than the appropriate nitrogen ligands. The complexes show rather low activity against E. coli.

Phenazine antibiotic inspired discovery of potent bromophenazine antibacterial agents against Staphylococcus aureus and Staphylococcus epidermidis

2014 ◽  
Vol 12 (6) ◽  
pp. 881-886 ◽  
Author(s):  
Nicholas V. Borrero ◽  
Fang Bai ◽  
Cristian Perez ◽  
Benjamin Q. Duong ◽  
James R. Rocca ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Staphylococcus Epidermidis ◽  
Antibacterial Agents

We have discovered a novel class of bromophenazines with potent antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis.

scholarly journals Binuclear Rhodium(II) Complexes With Selective Antibacterial Activity

1997 ◽  
Vol 4 (2) ◽  
pp. 81-88 ◽  
Author(s):  
Małgorzata Bień ◽  
Tadeusz M. Lachowicz ◽  
Agnieszka Rybka ◽  
Florian P. Pruchnik ◽  
Lilianna Trynda
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nmr Spectroscopy ◽  
Antibacterial Agents ◽  
Structure And Properties ◽  
E Coli ◽  
Nitrogen Ligands ◽  
And Staphylococcus Aureus ◽  
Low Activity

Binuclear rhodium(II) complexes [Rh2Cl2(μ-OOCR)2(N-N)2] {R = H, Me; N-N = 2,2'-bipyridine (bpy), 1,10-phenanthroline (phen)} and [Rh2(μ-OOCR)2(N-N)2(H2O)2](RCOO)2 (R = Me, Et;) have been synthesized and their structure and properties have been studied by electronic, IR and H1 NMR spectroscopy. Antibacterial activity of these complexes against Escherichia coli and Staphylococcus aureus has been investigated. The most active antibacterial agents against E. coli were [Rh2Cl2(μ-OOCR)2(N-N)2] and [Rh2(μ-OOCR)2(N-N)2(H2O)2](RCOO)2 {R = H and Me} which were considerably more active than the appropriate nitrogen ligands. The complexes show low activity against S. aureus. The activity of the complexes [Rh2(OOCR)2(N-N)2(H2O)2](OOCR)2 against E. coli decreases in the series: R=H≅CH3>C2H5>C3H7≅C4H9. The reverse order was found in the case of S. aureus.

Comparative Study of the Antimicrobial Effect of Different Antibiotics Mixed with CuO, MgO and ZnO Nanoparticles in Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli cultures

2014 ◽  
Vol 1675 ◽  
pp. 59-64
Author(s):  
Raúl Alenó ◽  
Anthony López Collazo ◽  
Eulalia Medina ◽  
Lourdes Díaz Figueroa ◽  
José I. Ramírez ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Cell Death ◽  
Optical Properties ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Antimicrobial Effect ◽  
Antibacterial Effects ◽  
New Methods

ABSTRACTDue to the rapid advance of the emergence of resistant microorganisms to different antibiotics, there is a need to create new antimicrobial agents. It is possible that Nanotechnology has a great impact in this area since the nanoparticles can improve the antimicrobial effect of the antibiotics. In this study we used three different metal oxides nanoparticles, the MgO, ZnO and CuO. These nanoparticles were selected because their interactions leading to cell death and their optical properties. The aim of this study is to develop new methods that are more effective against resistance bacteria, developing antibacterial agents using different nanoparticles against Escherichia coli (ATCC 10536), Pseudomonas aeruginosa (ATCC 10145), and Staphylococcus aureus (ATCC BAA-1026). This study was conducted to evaluate the antibacterial effects of a combination of nanoparticles together with different concentrations of three antibiotics, Gentamicin, Cephalexin and Co-Trimoxazole. The results showed that some nanoparticles are effective to inhibit growth in these microorganisms by increasing the effectiveness of the antibiotic. Therefore, the present study indicates that the combination of the nanoparticles with antibiotics may be applicable as a new antimicrobial agent.

scholarly journals Antibacterial Activity of Cinnamon Extract (Cinnamomum burmannii) against Staphylococcus aureus and Escherichia coli In Vitro

2019 ◽  
Vol 3 (2) ◽  
pp. 19-28
Author(s):  
Nita Parisa ◽  
Rahma Nur Islami ◽  
Ella Amalia ◽  
Mariana Mariana ◽  
Riana Sari Puspita Rasyid
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Ethanol Extract ◽  
Inhibition Zone ◽  
Control Group ◽  
Antibacterial Compounds ◽  
Cinnamon Extract ◽  
Cinnamomum Burmannii

Abstract   Infectious disease is one of the most common diseases in the world. Staphylococcus aureus and Escherichia coli are two common causes of infection and are resistant to many antibiotics, so the new agents are needed to overcome antibiotic resistance. Cinnamon is often used as a preservative because it has antibacterial activity. Cinnamomum burmannii is kind of native cinnamon from Indonesia. The antimicrobial active compounds cinnamaldehyde and eugenol are the main reasons for its antibacterial activity. This study observed the efficacy of the cinnamon extract (Cinnamomum burmannii) as antibacterial against Staphylococcus aureus and Escherichia coli. An experimental study, in vitro using Post-test Only Control Group Designed, has been done in Microbiology and Biotechnology Laboratory of Medical Faculty of Sriwijaya University. Cinnamon was extracted, then tested for its antibacterial activity using well diffusion and serial dilution to determine diameter of inhibition zone and minimum bactericidal concentration. Phytochemical tests were also conducted to determine the antibacterial compounds of cinnamon extract. Ethanol extract of cinnamon was able to inhibit the growth of Staphylococcus aureus with MBC 5% and inihibitory zone 6,84±0,68 mm and Escherichia coli with MBC 10% and inhibitory zone 5,69±0,69 mm. Cinnamon extract which has the greatest effectiveness is concentration of 40% with inhibition zone 15,69±0,80 mm (Staphylococcus aureus) and 9,63±0,59 mm (Escherichia coli). This ability is due to the antibacterial compounds as evidenced by positive results in various phytochemical tests. Cinnamon extract is effective as antibacterial against Staphylococcus aureus and Escherichia coli in vitro.   Keywords: efficacy, antibacterial, Cinnamomum burmannii, Staphylococcus aureus, Escherichia coli

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