scholarly journals Metal complexes as a promising source for new antibiotics

2020 ◽  
Vol 11 (10) ◽  
pp. 2627-2639 ◽  
Author(s):  
Angelo Frei ◽  
Johannes Zuegg ◽  
Alysha G. Elliott ◽  
Murray Baker ◽  
Stefan Braese ◽  
...  
Keyword(s):  
Antibiotic Resistance ◽  
Metal Complexes ◽  
Organic Molecules ◽  
Hit Rate ◽  
New Antibiotics ◽  
New Compounds ◽  
Eskape Pathogens ◽  
Promising Source

There is a dire need for new compounds to combat antibiotic resistance: metal complexes might provide the solution. 906 metal complexes were evaluated against dangerous ESKAPE pathogens and found to have a higher hit-rate than organic molecules.

scholarly journals Correction: Metal complexes as a promising source for new antibiotics

2020 ◽  
Vol 11 (17) ◽  
pp. 4531-4531 ◽  
Author(s):  
Angelo Frei ◽  
Johannes Zuegg ◽  
Alysha G. Elliott ◽  
Murray Baker ◽  
Stefan Braese ◽  
...  
Keyword(s):  
Metal Complexes ◽  
New Antibiotics ◽  
Promising Source

Correction for ‘Metal complexes as a promising source for new antibiotics’ by Angelo Frei et al., Chem. Sci., 2020, 11, 2627–2639.

scholarly journals Metal Complexes as a Promising Source for New Antibiotics

2019 ◽  
Author(s):  
Angelo Frei ◽  
Johannes Zuegg ◽  
Alysha Elliott ◽  
Murray Baker ◽  
Stefan Bräse ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Compounds ◽  
Chemical Structures ◽  
Mammalian Cell Lines ◽  
New Antibiotics ◽  
Antibiotic Compounds ◽  
Drug Pipeline ◽  
Promising Source ◽  
Derivatives Of ◽  
Nanomolar Range

There is a dire need for new classes of antimicrobial compounds to combat the growing threat of widespread antibiotic resistance. With a currently very scarce drug pipeline, consisting mostly of derivatives of known antibiotics, new classes of antibiotics are urgently required. Antibiotic compounds are notorious for not having very “drug-like” chemical structures. Metal complexes are currently in clinical development for the treatment of cancer, malaria and neurodegenerative diseases. However, only little attention has been paid to their application as potential antimicrobial compounds. We report the evaluation of 906 metal-containing compounds that have been screened by the Community for Open Antimicrobial Drug Discovery (CO-ADD) for antimicrobial activity. Metal-bearing compounds display a significantly higher hit-rate (9.9%) when compared to the purely organic molecules (0.87%) in the CO-ADD database. Out of 906 compounds, 88 show activity against at least one of the tested strains, including fungi, while not displaying any cytotoxicity against mammalian cell lines or haemolytic properties. Herein, we highlight the structures of the 30 compounds with activity against Gram-positive and/or Gram-negative bacteria containing Mn, Co, Zn, Ru, Ag, Eu, Ir and Pt, with activities down to the nanomolar range against methicillin resistant <i>S. aureus </i>(MRSA). This work reveals the vast diversity that metal-containing compounds can bring to antimicrobial research. It is important to raise awareness of these types of compounds for the design of truly novel antibiotics with potential for combatting antimicrobial resistance.

scholarly journals Essential Metabolic Routes as a Way to ESKAPE from Antibiotic Resistance

2019 ◽  
Author(s):  
Angélica Luana C. Barra ◽  
Lívia de Oliveira C. Dantas ◽  
Luana Galvão Morão ◽  
Raíssa F. Gutierrez ◽  
Igor Polikarpov ◽  
...  
Keyword(s):  
Antibiotic Resistance ◽  
Vitamin B1 ◽  
Basic Research ◽  
Resistant Bacteria ◽  
Biosynthesis Pathway ◽  
Acinetobacter Baumanii ◽  
Governmental Agencies ◽  
Current State ◽  
New Antibiotics ◽  
Eskape Pathogens

AbstractThe antibiotic resistance is a worldwide concern that requires a concerted action from physicians, patients, governmental agencies and academia to prevent infections and the spread of resistance, to track resistant bacteria, to improve the use of current antibiotics and to develop new antibiotics. Despite the efforts spent so far, the current antibiotics in the market are restricted to only five general targets/pathways highlighting the need for basic research focusing on the discovery and evaluation of new potential targets. Here we interrogate two biosynthetic pathways as potentially druggable pathways in bacteria. The biosynthesis pathway for thiamine (vitamin B1), absent in humans, but found in many bacteria, including organisms in the group of the ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanii, Pseudomonas aeruginosa and Enterobacter species) and the biosynthesis pathway for pyridoxal 5’-phosphate and its vitamers (vitamin B6), found in S. aureus. Using current genomic data, we discuss the possibilities of inhibition of enzymes in the pathway and review the current state of the art in the scientific literature.

scholarly journals Metal Complexes as a Promising Source for New Antibiotics

2019 ◽  
Author(s):  
Angelo Frei ◽  
Johannes Zuegg ◽  
Alysha Elliott ◽  
Murray Baker ◽  
Stefan Bräse ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Compounds ◽  
Chemical Structures ◽  
Mammalian Cell Lines ◽  
New Antibiotics ◽  
Antibiotic Compounds ◽  
Drug Pipeline ◽  
Promising Source ◽  
Derivatives Of ◽  
Nanomolar Range

There is a dire need for new classes of antimicrobial compounds to combat the growing threat of widespread antibiotic resistance. With a currently very scarce drug pipeline, consisting mostly of derivatives of known antibiotics, new classes of antibiotics are urgently required. Antibiotic compounds are notorious for not having very “drug-like” chemical structures. Metal complexes are currently in clinical development for the treatment of cancer, malaria and neurodegenerative diseases. However, only little attention has been paid to their application as potential antimicrobial compounds. We report the evaluation of 906 metal-containing compounds that have been screened by the Community for Open Antimicrobial Drug Discovery (CO-ADD) for antimicrobial activity. Metal-bearing compounds display a significantly higher hit-rate (9.9%) when compared to the purely organic molecules (0.87%) in the CO-ADD database. Out of 906 compounds, 88 show activity against at least one of the tested strains, including fungi, while not displaying any cytotoxicity against mammalian cell lines or haemolytic properties. Herein, we highlight the structures of the 30 compounds with activity against Gram-positive and/or Gram-negative bacteria containing Mn, Co, Zn, Ru, Ag, Eu, Ir and Pt, with activities down to the nanomolar range against methicillin resistant <i>S. aureus </i>(MRSA). This work reveals the vast diversity that metal-containing compounds can bring to antimicrobial research. It is important to raise awareness of these types of compounds for the design of truly novel antibiotics with potential for combatting antimicrobial resistance.

scholarly journals Metal Complexes as a Promising Source for New Antibiotics

2019 ◽  
Author(s):  
Angelo Frei ◽  
Johannes Zuegg ◽  
Alysha Elliott ◽  
Murray Baker ◽  
Stefan Bräse ◽  
...  
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Compounds ◽  
Chemical Structures ◽  
Mammalian Cell Lines ◽  
New Antibiotics ◽  
Antibiotic Compounds ◽  
Drug Pipeline ◽  
Promising Source ◽  
Derivatives Of ◽  
Nanomolar Range

There is a dire need for new classes of antimicrobial compounds to combat the growing threat of widespread antibiotic resistance. With a currently very scarce drug pipeline, consisting mostly of derivatives of known antibiotics, new classes of antibiotics are urgently required. Antibiotic compounds are notorious for not having very “drug-like” chemical structures. Metal complexes are currently in clinical development for the treatment of cancer, malaria and neurodegenerative diseases. However, only little attention has been paid to their application as potential antimicrobial compounds. We report the evaluation of 906 metal-containing compounds that have been screened by the Community for Open Antimicrobial Drug Discovery (CO-ADD) for antimicrobial activity. Metal-bearing compounds display a significantly higher hit-rate (9.9%) when compared to the purely organic molecules (0.87%) in the CO-ADD database. Out of 906 compounds, 88 show activity against at least one of the tested strains, including fungi, while not displaying any cytotoxicity against mammalian cell lines or haemolytic properties. Herein, we highlight the structures of the 30 compounds with activity against Gram-positive and/or Gram-negative bacteria containing Mn, Co, Zn, Ru, Ag, Eu, Ir and Pt, with activities down to the nanomolar range against methicillin resistant <i>S. aureus </i>(MRSA). This work reveals the vast diversity that metal-containing compounds can bring to antimicrobial research. It is important to raise awareness of these types of compounds for the design of truly novel antibiotics with potential for combatting antimicrobial resistance.

scholarly journals Antibacterial Compounds from Mushrooms: A Lead to Fight ESKAPEE Pathogenic Bacteria?

Planta Medica ◽  
2020 ◽  
Author(s):  
Violette Hamers ◽  
Clément Huguet ◽  
Mélanie Bourjot ◽  
Aurélie Urbain
Keyword(s):  
Antibiotic Resistance ◽  
Global Health ◽  
Pathogenic Bacteria ◽  
Resistance Mechanisms ◽  
Pathogenic Microorganisms ◽  
Bacterial Strains ◽  
Antibacterial Compounds ◽  
New Antibiotics ◽  
Hospital Stays ◽  
Antibacterial Potential

AbstractInfectious diseases are among the greatest threats to global health in the 21st century, and one critical concern is due to antibiotic resistance developed by an increasing number of bacterial strains. New resistance mechanisms are emerging with many infections becoming more and more difficult if not impossible to treat. This growing phenomenon not only is associated with increased mortality but also with longer hospital stays and higher medical costs. For these reasons, there is an urgent need to find new antibiotics targeting pathogenic microorganisms such as ESKAPEE bacteria. Most of currently approved antibiotics are derived from microorganisms, but higher fungi could constitute an alternative and remarkable reservoir of anti-infectious compounds. For instance, pleuromutilins constitute the first class of antibiotics derived from mushrooms. However, macromycetes still represent a largely unexplored source. Publications reporting the antibacterial potential of mushroom extracts are emerging, but few purified compounds have been evaluated for their bioactivity on pathogenic bacterial strains. Therefore, the aim of this review is to compile up-to-date data about natural products isolated from fruiting body fungi, which significantly inhibit the growth of ESKAPEE pathogenic bacteria. When available, data regarding modes of action and cytotoxicity, mandatory when considering a possible drug development, have been discussed in order to highlight the most promising compounds.

scholarly journals Carbonic Anhydrase Inhibitors Part 721 Synthesis and Antiglaucoma Properties of Metal Complexes of p-Fluorobenzolamide

1999 ◽  
Vol 6 (2) ◽  
pp. 67-73 ◽  
Author(s):  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Luca Menabuoni ◽  
Francesco Mincione ◽  
Fabrizio Briganti ◽  
...  
Keyword(s):  
Intraocular Pressure ◽  
Carbonic Anhydrase ◽  
Metal Ions ◽  
Metal Complexes ◽  
Carbonic Anhydrase Inhibitors ◽  
Physico Chemical ◽  
New Compounds

Metal complexes of a heterocyclic sulfonamides possessing very strong carbonic anhydrase (CA) inhibitory properties, i.e., 5-(p-fluorobenzenesulfonylamido)-1,3,4-thiadiazole-2-sulfonamide (p-fluorobenzolamide) were prepared. The new complexes contained metal ions such as Zn(II), Cu(II), Co(II), Ni(II), Cd(II) and Mn(II). The new compounds were characterized by standard physico-chemical procedures, and assayed as inhibitors of three CA isozymes, CA I, II and IV. Very good inhibition has been evidenced both for the parent sulfonamides as well as for the prepared complexes, against all three investigated isozymes. Some of these new complexes as well as the parent sulfonamide, strongly lowered intraocular pressure (IOP) in normotensive rabbits when administered as a 2% solution into the eye.

Recent progress in the mechanochromism of phosphorescent organic molecules and metal complexes

2016 ◽  
Vol 4 (28) ◽  
pp. 6688-6706 ◽  
Author(s):  
Pengchong Xue ◽  
Jipeng Ding ◽  
Panpan Wang ◽  
Ran Lu
Keyword(s):  
Metal Complexes ◽  
Recent Progress ◽  
Organic Molecules ◽  
Mechanical Force ◽  
Spectral Shifts ◽  
Luminescence Color

Phosphorescent mechanochromic materials may change their luminescence color and intensity with large spectral shifts under a mechanical force stimulus.

scholarly journals Discovering the Hidden Secondary Metabolome of Myxococcus xanthus: a Study of Intraspecific Diversity

2008 ◽  
Vol 74 (10) ◽  
pp. 3058-3068 ◽  
Author(s):  
Daniel Krug ◽  
Gabriela Zurek ◽  
Ole Revermann ◽  
Michiel Vos ◽  
Gregory J. Velicer ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Myxococcus Xanthus ◽  
Single Species ◽  
Intraspecific Diversity ◽  
Metabolic Diversity ◽  
Model Species ◽  
Metabolite Profiles ◽  
High Level ◽  
New Compounds ◽  
Promising Source

ABSTRACT As a monophyletic group, the myxobacteria are known to produce a broad spectrum of secondary metabolites. However, the degree of metabolic diversity that can be found within a single species remains unexplored. The model species Myxococcus xanthus produces several metabolites also present in other myxobacterial species, but only one compound unique to M. xanthus has been found to date. Here, we compare the metabolite profiles of 98 M. xanthus strains that originate from 78 locations worldwide and include 20 centimeter-scale isolates from one location. This screen reveals a strikingly high level of intraspecific diversity in the M. xanthus secondary metabolome. The identification of 37 nonubiquitous candidate compounds greatly exceeds the small number of secondary metabolites previously known to derive from this species. These results suggest that M. xanthus may be a promising source of future natural products and that thorough intraspecific screens of other species could reveal many new compounds of interest.

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