A5041202179- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- N-Heterocyclic Carbenes in Organic and Inorganic Chemistry
- Catalytic Cross-Coupling Reactions
- Synthesis and Biological Evaluation
- Antifungal resistance and susceptibility
- Ferrocene Chemistry and Applications
- Synthetic Organic Chemistry Methods
- Catalytic Alkyne Reactions
- Redox biology and oxidative stress
- Enzyme function and inhibition
- Pneumocystis jirovecii pneumonia detection and treatment
- Gut microbiota and health
- Antimicrobial agents and applications
- Fungal Infections and Studies
- Peptidase Inhibition and Analysis
- Organoboron and organosilicon chemistry
- Quinazolinone synthesis and applications
- Bacterial biofilms and quorum sensing
- Asymmetric Hydrogenation and Catalysis
- Click Chemistry and Applications
- Metal complexes synthesis and properties
Université Paris Sciences et Lettres
2023
Centre National de la Recherche Scientifique
2023
University College Dublin
2016-2023
Chimie ParisTech
2023
Technische Universität Braunschweig
2023
The urgent need to combat antibiotic resistance and develop novel antimicrobial therapies has triggered studies on metal-based formulations. N-heterocyclic carbene (NHC) complexes coordinate transition metals generate a broad range of anticancer and/or agents, with ongoing efforts being made enhance the lipophilicity drug stability. lead silver(I) acetate complex, 1,3-dibenzyl-4,5-diphenylimidazol-2-ylidene (NHC*) (SBC3), previously demonstrated promising growth biofilm-inhibiting...
The ongoing SARS-CoV-2 pandemic has caused a high demand for novel innovative antiviral drug candidates. Despite promising results, metal complexes have been relatively unexplored as agents in general and particular against SARS-CoV-2. Here we report on silver NHC with chloride or iodide counter ligands that are potent inhibitors of the papain-like protease (PLpro) but inactive 3C-like (3CLpro) another protease. Mechanistic studies selected complex confirmed zinc removal from binding domain...
The anticancer drug candidate 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene gold(I) chloride (NHC-AuCl) and its 2',3',4',6'-tetra-O-acetyl-β-D-glucopyranosyl-1'-thiolate derivative (NHC-AuSR), which is a potential ligand for glucose transporters, were tested on the NCI 60 cancer cell panel in vitro. NHC-AuCl NHC-AuSR showed very good activity against wide range of human lines inclusive renal with similar average GI50 values 1.78 1.95 μM, respectively. This encouraged maximum tolerable dose...
Antibiotic resistance is a growing problem for public health and associated with increasing economic costs mortality rates. Silver silver-related compounds have been used centuries due to their antimicrobial properties. In this work, we show that 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene silver(I) acetate/NHC*-Ag-OAc (SBC3) reversible, high affinity inhibitor of E. coli thioredoxin reductase (TrxR; Ki =10.8±1.2 nM). Minimal inhibition concentration (MIC) tests different P. aeruginosa...
The anticancer drug candidates 1,3-dibenzyl-4,5-diphenyl-imidazol-2-ylidene gold(I) dimethylamino dithiocarbamate and 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosyl-1-thiolate derivative exhibited nanomolar in-vitro activity against prostate cancer cells advanced (PC3) micromolar inhibition of mammalian thioredoxin reductase. Encouraging maximum tolerable dose experiments led to human subcutaneous xenograft experiments; were applied twelve times at two doses in groups n = 5 PC3 tumor-bearing...
N-heterocyclic silver carbene compounds have been extensively studied and shown to be active agents against a host of pathogenic bacteria fungi. By incorporating hypothesized virulence targeting substituents into NHC-silver systems via salt metathesis, an atom-efficient complexation process can used develop new complexes target the passive microbial cell. The incorporation fatty acids FtsZ inhibitor achieved, creation both intermediate subsequent complex has streamlined continuous flow...
Drug resistance observed with many anti-infectives clearly highlights the need for new broad-spectrum agents to treat especially neglected tropical diseases (NTDs) caused by eukaryotic parasitic pathogens, including fungal infections. Herein, we show that simple modification of one most well-known antifungal drugs, fluconazole, organometallic moieties not only improves activity parent drug but also broadens scope application derivatives. These compounds were highly effective in vivo against...
Abstract The antimicrobial properties of silver have been exploited for many centuries and continue to gain interest in the fight against drug resistance. broad-spectrum activity low toxicity led its incorporation into a wide range novel agents, including N-heterocyclic carbene (NHC) complexes. vivo efficacy NHC silver(I) acetate complex SBC3, derived from 1,3-dibenzyl-4,5-diphenylimidazol-2-ylidene (NHC*), previously demonstrated, although mode(s) action SBC3 remains be fully elucidated....
Gold monochloride and monobromide can be transformed into monomeric complexes by ligands such as CO, PPh3 or Me2S, ligand-stabilized gold compounds have been investigated catalysts, luminescent materials anticancer drugs, especially when coordinated to a lipophilic benzyl-substituted N-heterocyclic carbene (NHC) ligand. The triclinic structures of NHC-Au-Cl {chlorido(1,3-dibenzyl-4,5-diphenylimidazol-2-ylidene)gold, [AuCl(C29H24N2)]} NHC-Au-Br...
Drug resistance observed with many anti-infectives clearly highlights the need for new broad-spectrum agents to treat especially neglected tropical diseases (NTDs) caused by eukaryotic parasitic pathogens including fungal infections. Since these target most vulnerable communities who are disadvantaged health and socio-economic factors, should be, if possible, easy-to-prepare allow commercialization based on their low cost. In this study, we show that simple modification of one well-known...