Article
Chemistry, Medicinal
Dilek Turker, Elvan Ustun, Selami Gunal, Hatice Yildiz, Serpil D. Dusunceli, Ismail Ozdemir
Summary: New N-heterocyclic carbene precursors and silver-NHC complexes were synthesized and characterized, showing promising antibacterial activities against standard bacterial and fungal strains. The compounds were also analyzed using density functional theory (DFT)/time-dependent DFT and docking methods.
ARCHIV DER PHARMAZIE
(2022)
Article
Chemistry, Inorganic & Nuclear
Deniz Demir Atli, Didem Aksu
Summary: A new benzimidazolium salt containing a 2,5-dimethylbenzyl substituent and six N-heterocyclic carbene (NHC) silver complexes were synthesized and characterized. The stability of the complexes in solution was investigated, and their antibacterial activities against Gram-positive and Gram-negative bacteria were evaluated. Among the complexes, 2b exhibited the highest antibacterial activity overall.
JOURNAL OF COORDINATION CHEMISTRY
(2023)
Review
Chemistry, Multidisciplinary
Zikun Wang, Nikolaos V. Tzouras, Steven P. Nolan, Xihe Bi
Summary: Silver N-heterocyclic carbenes (Ag-NHCs) have good biocompatibility and are widely used in medicine and coordination chemistry, but their coordination with silver can weaken the Lewis acidity of Ag(I), resulting in slow development as catalysts. Future opportunities lie in further research on the catalytic mechanisms of Ag-NHCs to enhance their catalytic activity.
TRENDS IN CHEMISTRY
(2021)
Article
Chemistry, Physical
Qing Wu, Rui Peng, Fang Gong, Yufeng Luo, Hean Zhang, Qianling Cui
Summary: In this study, we successfully synthesized hydrophilic AuNCs in an aqueous medium using a NHC-based ligand as both a reducing agent and stabilizer. These AuNCs, with their ultrasmall size and positively charged surface, can penetrate bacterial cell walls and accumulate in bacteria, leading to an increase in intracellular reactive oxygen species. As a result, these AuNCs exhibit wide-spectrum antibacterial activity.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2022)
Article
Chemistry, Applied
Weihong Zheng, Qing Zheng, Chao Chen, Hangxiang Wang
Summary: Three silver N-heterocyclic carbene complexes were synthesized and showed strong antitumor activity, with Ag2 exhibiting the highest cytotoxicity; the complexes induced intracellular reactive oxygen species overproduction and mitochondrial dysfunction.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Chemistry, Applied
Thomas Scattolin, Petra Lippmann, Marek Belis, Kristof van Hecke, Ingo Ott, Steven P. Nolan
Summary: A straightforward synthetic route to new N-heterocyclic carbene (NHC)-gold-steroidyl complexes is reported, which displayed good cytotoxicity against cancer cells.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Review
Chemistry, Organic
Mohammed Sharique, Uttam K. Tambar
Summary: Aromatic compounds are commonly used in pharmaceuticals and functional materials, leading to a focus on synthetic methods for constructing highly functionalized aromatic frameworks from acyclic precursors. Transition metal catalysis and base-promoted benzannulation reactions are widely utilized for this purpose. Recently, organocatalytic approaches such as N-heterocyclic carbene catalysis have emerged as efficient tools for the formation of complexly substituted aryl rings under mild reaction conditions.
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Physical
Xiaokang Lv, Jun Xu, Cuiyun Sun, Fen Su, Yuanlin Cai, Zhichao Jin, Yonggui Robin Chi
Summary: Ferrocene-derived dicarbaldehydes with pro-chiral planes can be desymmetrized under the catalysis of chiral Nheterocyclic carbene organic catalysts, resulting in enantiomerically enriched planar chiral ferrocene products. The reaction selectively activates and reacts with one aldehyde moiety while leaving the other untouched. The obtained products show potential applications as catalysts in chemical synthesis and for antimicrobial activities in pesticide development.
Article
Chemistry, Inorganic & Nuclear
Orhi Esarte Palomero, Ashley L. Cunningham, Bryan W. Davies, Richard A. Jones
Summary: Three new coinage metal carbene complexes of silver and gold synthesized from a thiamine inspired proligand were characterized and found to exhibit potent antimicrobial activity, with the gold carbene derivative showing the strongest activity against Gram-positive methicillin-resistant Staphylococcus aureus (MRSA) in MIC studies.
INORGANICA CHIMICA ACTA
(2021)
Article
Chemistry, Multidisciplinary
Hang Shen, Michael B. Larsen, Allison G. Roessler, Paul M. Zimmerman, Andrew J. Boydston
Summary: A new flex-activated mechanophore has been discovered, which releases an N-heterocyclic carbene (NHC) under mechanical load. This design demonstrates a promising first step towards flex-activated designs with downstream reactivities, allowing for iterative activation increases in the material through non-destructive compression cycles. The potential modularity of the mechanophore design is highlighted by the demonstration of two different NHC structures.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Inorganic & Nuclear
Mert Olgun Karatas, Tuba Keskin, Namik Ozdemir, Hasan Kucukbay, Suat Tekin, Ahmet Mansur, Selami Gunal, Suleyman Sandal
Summary: In this study, Ag, Rh, and Ir complexes of a silyl-substituted NHC ligand were synthesized and their biological properties were investigated. The results showed that these complexes exhibited comparable or better cytotoxicity against cancer cells and antimicrobial activity compared to standard drugs.
INORGANIC CHEMISTRY COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Zhen Li, Pengju Ji, Jin-Pei Cheng
Summary: A Brønsted basicity scale was established for nine representative N-heterocyclic olefins (NHOs) using an UV-visible spectroscopic method. The unsaturated NHOs were found to have stronger basicities compared to their N-heterocyclic carbene (NHC) analogues, while the basicities of the saturated NHOs were weaker. The nucleophilicity of the NHOs was also stronger than commonly used Lewis bases but weaker than their NHC analogues.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Gianmarco Pisano, Catherine S. J. Cazin
Summary: A user-friendly and highly efficient mechanochemical strategy for the synthesis of well-defined, catalytically relevant N-heterocyclic carbene-metal complexes is reported. The protocol yields good to excellent results and minimizes solvent usage by only using environmentally benign solvents in the purification step.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2021)
Article
Chemistry, Multidisciplinary
Ludwig Zapf, Udo Radius, Maik Finze
Summary: The paper describes the synthesis of 1,3-bis(tricyanoborane)imidazolate anion and its derivatives, including a novel dianionic N-heterocyclic carbene. These compounds exhibit unique electronic and steric properties, making them promising ligands and building blocks for coordination chemistry.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Multidisciplinary
Junbeom Park, Jaelim Kim, Gu Yoon Jeong, Youngsuk Kim, Eunsung Lee
Summary: This study investigates the electron and proton transfer chemistry of N-heterocyclic carbene nitric oxide radical compounds and prepares a variety of nitrosyl derivatives. The reactions of these derivatives resemble those of transition metal nitrosyl complexes.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2023)
Review
Biotechnology & Applied Microbiology
Yann Thierry Le Guen, Tony Le Gall, Patrick Midoux, Philippe Guegan, Serge Braun, Tristan Montier
JOURNAL OF GENE MEDICINE
(2020)
Article
Biochemistry & Molecular Biology
Bazoly Rasolonjatovo, Nicolas Illy, Veronique Bennevault, Jerome Mathe, Patrick Midoux, Tony Le Gall, Thomas Haudebourg, Tristan Montier, Pierre Lehn, Bruno Pitard, Herve Cheradame, Cecile Huin, Philippe Guegan
MACROMOLECULAR BIOSCIENCE
(2020)
Review
Pharmacology & Pharmacy
Rosy Ghanem, Veronique Laurent, Philippe Roquefort, Tanguy Haute, Sophie Ramel, Tony Le Gall, Thierry Aubry, Tristan Montier
Summary: The respiratory epithelium is susceptible to diseases like cystic fibrosis, which impact airway function. Artificial mucus models play a crucial role in evaluating gene transfer systems' effectiveness in reaching the epithelium.
Article
Medicine, General & Internal
Y. T. Le Guen, T. Le Gall, V Laurent, F. D'Arbonneau, S. Braun, T. Montier
Summary: Duchenne muscular dystrophy is a common type of muscular dystrophy caused by mutations in the dystrophin gene, leading to a lower life span and quality of life compared to the general population. New therapeutic approaches are being investigated to provide new perspectives and hope for the care of this severe disease.
BULLETIN DE L ACADEMIE NATIONALE DE MEDECINE
(2021)
Article
Medicine, Research & Experimental
Yann T. Le Guen, Chantal Pichon, Philippe Guegan, Kevin Pluchon, Tanguy Haute, Sandrine Quemener, Juliette Ropars, Patrick Midoux, Tony Le Gall, Tristan Montier
Summary: The study focuses on the enhanced nuclear import of plasmid DNA carrying 3NF sequences through interaction with NF-kappa B. Results show modest to substantial advantages for 3NF-equipped pDNA in both in vitro and in vivo gene transfer applications, emphasizing the potential of optimized nuclear import for efficient non-viral gene transfer.
MOLECULAR THERAPY-NUCLEIC ACIDS
(2021)
Article
Cell Biology
Rosy Ghanem, Philippe Roquefort, Sophie Ramel, Veronique Laurent, Tanguy Haute, Tony Le Gall, Thierry Aubry, Tristan Montier
Summary: The mucus in CF patients' airways is a yield stress fluid with unique rheological properties. Rheological analyses can provide biophysical markers for disease management. Treatment with rhDNAse appears to lower the apparent yield stress of CF sputum, which could be a predictive biomarker for prognosis and aid in the development of new mucolytic agents.
Article
Pharmacology & Pharmacy
Tony Le Gall, Mathieu Berchel, Lee Davies, Angelique Mottais, Rosy Ghanem, Alain Fautrel, Deborah Gill, Steve Hyde, Pierre Lehn, Jean-Marie Lehn, Loic Lemiegre, Thierry Benvegnu, Paul-Alain Jaffres, Bruno Pitard, Tristan Montier
Summary: Aerosol lung gene therapy using non-viral delivery systems shows promise as a therapeutic strategy for chronic respiratory diseases. This study demonstrates that lipidic aminoglycoside derivative-based formulations possess efficient lung transfection activity following aerosol delivery, suggesting their potential as alternatives to GL67A.
Review
Pharmacology & Pharmacy
Raphaelle Youf, Max Mueller, Ali Balasini, Franck Thetiot, Mareike Mueller, Alize Hascoet, Ulrich Jonas, Holger Schoenherr, Gilles Lemercier, Tristan Montier, Tony Le Gall
Summary: Antimicrobial photodynamic therapy (aPDT) has become a fundamental tool in modern therapeutics, with the ability to treat localized infections by combining various photosensitizers and other antimicrobial treatments. This review summarizes the latest advances in aPDT applications and discusses developments in photochemistry, photophysics, and carrier systems.
Article
Engineering, Biomedical
Zhiyuan Jia, Mareike Mueller, Tony Le Gall, Martijn Riool, Max Mueller, Sebastian A. J. Zaat, Tristan Montier, Holger Schoenherr
Summary: This study developed color-encoded chitosan hydrogels for rapid and sensitive detection of bacterial enzymes and differentiating bacterial strains. The hydrogels with three different colorimetric enzyme substrates can detect and differentiate alpha-glucosidase, beta-galactosidase, and beta-glucuronidase, showing potential for point-of-care microbiological diagnostics in food safety and medical settings.
BIOACTIVE MATERIALS
(2021)
Article
Immunology
Jiwar Al-Zawity, Faria Afzal, Aysha Awan, Daniela Nordhoff, Alexander Kleimann, Daniel Wesner, Tristan Montier, Tony Le Gall, Mareike Muller
Summary: This study investigates the influence of the steroid sex hormone estradiol (E-2) on biofilm formation of Pseudomonas aeruginosa in cystic fibrosis (CF) patients. The results show that E-2 treatment can increase the attached biofilm mass, remodel the biofilm ultrastructure, and potentially modulate the QS signaling in the biofilm.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Raphaelle Youf, Adeel Nasir, Mareike Mueller, Franck Thetiot, Tanguy Haute, Rosy Ghanem, Ulrich Jonas, Holger Schoenherr, Gilles Lemercier, Tristan Montier, Tony Le Gall
Summary: Antimicrobial photodynamic therapy (aPDT) is a treatment method that relies on various parameters. In this study, the application of Ruthenium(II) polypyridyl ([Ru(II)]) complexes in the airways of Cystic Fibrosis (CF) patients was investigated, and the influence of different parameters on their properties was studied. The results provide significant evidence for the clinical relevance of [Ru(II)]-based aPDT in CF lung airways.
Article
Pharmacology & Pharmacy
Rosy Ghanem, Mathieu Berchel, Tanguy Haute, Xavier Buin, Veronique Laurent, Raphaelle Youf, Amal Bouraoui, Tony Le Gall, Paul-Alain Jaffres, Tristan Montier
Summary: In cystic fibrosis gene therapy, aerosolization of genetic materials is the most relevant delivery strategy to reach the airway epithelium. This study compared the efficiency of gene delivery by aerosolization of two formulations: BSV163-based and b-PEI-based. Results showed that the DOPE ratio of the BSV163-based formulations influenced their ability to mediate high transfection efficacies.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Chemistry, Organic
Amal Bouraoui, Rosy Ghanem, Mathieu Berchel, Laure Deschamps, Veronique Vie, Gilles Paboeuf, Tony Le Gall, Tristan Montier, Paul-Alain Jaffres
ORGANIC & BIOMOLECULAR CHEMISTRY
(2020)
Article
Pharmacology & Pharmacy
Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa
Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
Article
Pharmacology & Pharmacy
James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner
Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)