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Inorganic and Organometallic Compounds as Antiparasitic, Antibacterial, and Antifungal Agents

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

Deadline for manuscript submissions: closed (31 January 2021) | Viewed by 13321

Special Issue Editor


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Guest Editor
Department of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, CH-3012 Bern, Switzerland
Interests: nuclear magnetic resonance; bioorganometallic chemistry; bioinorganic chemistry

Special Issue Information

Dear Colleagues,

Organometallic complexes have been used in cancer drug development for many years and, more recently, the potential of organometallic-based drug candidates against bacteria, parasites, and fungi has been demonstrated. In particular, the occurrence of multidrug-resistant bacteria has become an issue of such importance that the major pharmaceuticals companies have decided to join their forces on a special program worth $1 billion toward the development of new antimicrobial compounds. This program is unlike any witnessed to date in the fight against fungi and parasites, though the manifestation of multidrug-resistant parasites and fungi is certain to be problematic in the near future. Undoubtedly, the development of new classes of compounds to control the virulence of these pathogens is therefore urgently required.

This Special Issue is dedicated to sharing recent advances in the preparation of organometallic compounds as new classes of antibacterial, antifungal, and antiparasitic agents with potential for clinical development. I am confident that the knowledge we will gain from this Special Issue will help researchers to design future compounds which are able to match the steadily more demanding requirements laid down by regulatory agencies for compounds to rightly achieve the optimal balance of efficacy and safety.

Prof. Dr. Julien Furrer
Guest Editor

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Keywords

  • Organometallic compounds
  • Antiparasitic activity
  • Mechanisms of action
  • Biological targets
  • Resistance
  • Antibacterial
  • Antimicrobial
  • Antifungal

Published Papers (4 papers)

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Research

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18 pages, 1948 KiB  
Article
New Mononuclear and Binuclear Cu(II), Co(II), Ni(II), and Zn(II) Thiosemicarbazone Complexes with Potential Biological Activity: Antimicrobial and Molecular Docking Study
by Ahmed Gaber, Moamen S. Refat, Arafa A.M. Belal, Ibrahim M. El-Deen, Nader Hassan, Rozan Zakaria, Majid Alhomrani, Abdulhakeem S. Alamri, Walaa F. Alsanie and Essa M. Saied
Molecules 2021, 26(8), 2288; https://doi.org/10.3390/molecules26082288 - 15 Apr 2021
Cited by 55 | Viewed by 3656
Abstract
Herein, we report the synthesis of eight new mononuclear and binuclear Co2+, Ni2+, Cu2+, and Zn2+ methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and [...] Read more.
Herein, we report the synthesis of eight new mononuclear and binuclear Co2+, Ni2+, Cu2+, and Zn2+ methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and its metal complexes was fully characterized by elemental analysis, spectroscopic techniques (NMR, FTIR, UV-Vis), molar conductivity, thermogravimetric analysis (TG), and thermal differential analysis (DrTGA). The spectral and analytical data revealed that the obtained thiosemicarbazone-metal complexes have octahedral geometry around the metal center, except for the Zn2+-thiosemicarbazone complexes, which showed a tetrahedral geometry. The antibacterial and antifungal activities of the MTSC ligand and its (Co2+, Ni2+, Cu2+, and Zn2+) metal complexes were also investigated. Interestingly, the antibacterial activity of MTSC- metal complexes against examined bacteria was higher than that of the MTSC alone, which indicates that metal complexation improved the antibacterial activity of the parent ligand. Among different metal complexes, the MTSC- mono- and binuclear Cu2+ complexes showed significant antibacterial activity against Bacillus subtilis and Proteus vulgaris, better than that of the standard gentamycin drug. The in silico molecular docking study has revealed that the MTSC ligand could be a potential inhibitor for the oxidoreductase protein. Full article
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19 pages, 6516 KiB  
Article
Ruthenium(IV) Complexes as Potential Inhibitors of Bacterial Biofilm Formation
by Agnieszka Jabłońska-Wawrzycka, Patrycja Rogala, Grzegorz Czerwonka, Sławomir Michałkiewicz, Maciej Hodorowicz and Paweł Kowalczyk
Molecules 2020, 25(21), 4938; https://doi.org/10.3390/molecules25214938 - 26 Oct 2020
Cited by 7 | Viewed by 1994
Abstract
With increasing antimicrobial resistance there is an urgent need for new strategies to control harmful biofilms. In this study, we have investigated the possibility of utilizing ruthenium(IV) complexes (H3O)2(HL1)2[RuCl6]·2Cl·2EtOH (1) and [RuCl4 [...] Read more.
With increasing antimicrobial resistance there is an urgent need for new strategies to control harmful biofilms. In this study, we have investigated the possibility of utilizing ruthenium(IV) complexes (H3O)2(HL1)2[RuCl6]·2Cl·2EtOH (1) and [RuCl4(CH3CN)2](L32)·H2O (2) (where L1-2-hydroxymethylbenzimadazole, L32-1,4-dihydroquinoxaline-2,3-dione) as effective inhibitors for biofilms formation. The biological activities of the compounds were explored using E. coli, S. aureus, P. aeruginosa PAO1, and P. aeruginosa LES B58. The new chloride ruthenium complexes were characterized by single-crystal X-ray diffraction analysis, Hirshfeld surface analysis, FT-IR, UV-Vis, magnetic and electrochemical (CV, DPV) measurements, and solution conductivity. In the obtained complexes, the ruthenium(IV) ions possess an octahedral environment. The intermolecular classical and rare weak hydrogen bonds, and π···π stacking interactions significantly contribute to structure stabilization, leading to the formation of a supramolecular assembly. The microbiological tests have shown complex 1 exhibited a slightly higher anti-biofilm activity than that of compound 2. Interestingly, electrochemical studies have allowed us to determine the relationship between the oxidizing properties of complexes and their biological activity. Probably the mechanism of action of 1 and 2 is associated with generating a cellular response similar to oxidative stress in bacterial cells. Full article
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17 pages, 1030 KiB  
Article
Synthesis and Antimicrobial Evaluation of Some New Organic Tellurium Compounds Based on Pyrazole Derivatives
by Asmaa B. Sabti, Adil A. Al-Fregi and Majeed Y. Yousif
Molecules 2020, 25(15), 3439; https://doi.org/10.3390/molecules25153439 - 29 Jul 2020
Cited by 9 | Viewed by 2153
Abstract
A novel series of organic tellurium compounds based on pyrazole derivatives with a general formula of ArTeBr3 and Ar2TeBr2 [Ar = 2-(3-(4-substituted phenyl)-5-(2-chlorophenyl)-1H-pyrazol-1-yl)-3,5-dinitrophenyl] were obtained by the refluxing of corresponding aryl mercuric chlorides with TeBr4 in [...] Read more.
A novel series of organic tellurium compounds based on pyrazole derivatives with a general formula of ArTeBr3 and Ar2TeBr2 [Ar = 2-(3-(4-substituted phenyl)-5-(2-chlorophenyl)-1H-pyrazol-1-yl)-3,5-dinitrophenyl] were obtained by the refluxing of corresponding aryl mercuric chlorides with TeBr4 in two different mole ratio of 1:1 and 2:1, respectively, in free-moisture dioxane solvent under an argon atmosphere. Compounds of ArTeBr3 and Ar2TeBr2 were reduced by the action of ethanolic solution of hydrazine hydrate obtained Ar2Te2 and Ar2Te, respectively. Reaction of Ar2Te2 with excess thionyl chloride or iodine gave the corresponding trihalides ArTeCl3 and ArTeI3, respectively while the reaction of Ar2Te with thionyl chloride or iodine gave the corresponding Ar2TeCl3 and Ar2TeI3, respectively. The structures were elucidated according to their elemental analysis of carbon, hydrogen and nitrogen (CHN) and some of the spectroscopic techniques such as infrared IR and nuclear magnetic resonance for 1H and 13C. The antimicrobial activity for all the synthetic compounds were assayed against both Gram-negative and Gram-positive bacteria by using the agar diffusion method. The tellurated pyrazole derivatives showed a good degree against bacteria growth. In some cases, the antimicrobial activities of the synthetic compounds were better than amoxicillin. Full article
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Review

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31 pages, 9901 KiB  
Review
Recent Advances in the Biological Investigation of Organometallic Platinum-Group Metal (Ir, Ru, Rh, Os, Pd, Pt) Complexes as Antimalarial Agents
by Mziyanda Mbaba, Taryn M. Golding and Gregory S. Smith
Molecules 2020, 25(22), 5276; https://doi.org/10.3390/molecules25225276 - 12 Nov 2020
Cited by 25 | Viewed by 4720
Abstract
In the face of the recent pandemic and emergence of infectious diseases of viral origin, research on parasitic diseases such as malaria continues to remain critical and innovative methods are required to target the rising widespread resistance that renders conventional therapies unusable. The [...] Read more.
In the face of the recent pandemic and emergence of infectious diseases of viral origin, research on parasitic diseases such as malaria continues to remain critical and innovative methods are required to target the rising widespread resistance that renders conventional therapies unusable. The prolific use of auxiliary metallo-fragments has augmented the search for novel drug regimens in an attempt to combat rising resistance. The development of organometallic compounds (those containing metal-carbon bonds) as antimalarial drugs has been exemplified by the clinical development of ferroquine in the nascent field of Bioorganometallic Chemistry. With their inherent physicochemical properties, organometallic complexes can modulate the discipline of chemical biology by proffering different modes of action and targeting various enzymes. With the beneficiation of platinum group metals (PGMs) in mind, this review aims to describe recent studies on the antimalarial activity of PGM-based organometallic complexes. This review does not provide an exhaustive coverage of the literature but focusses on recent advances of bioorganometallic antimalarial drug leads, including a brief mention of recent trends comprising interactions with biomolecules such as heme and intracellular catalysis. This resource can be used in parallel with complementary reviews on metal-based complexes tested against malaria. Full article
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