Article
Chemistry, Multidisciplinary
Gaoji Wang, Goran Angelovski
Summary: A novel Gd3+ chelate has been developed that can selectively recognize Zn2+ and exhibit a significant increase in longitudinal relaxivity, representing a new momentum in developing suitable contrast agents for functional molecular imaging studies of Zn2+.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Article
Chemistry, Multidisciplinary
Jing Sun, Xutao Ma, Rongye Li, Min Lin, Lilei Shu, Xuesi Chen
Summary: This research developed a new type of antibacterial agents by preparing pH-dependent nanostructured assemblies from cationic copolypeptoid. The fiber-like micelles demonstrated better antimicrobial performance and efficacy against biofilms, showing high selectivity.
Article
Chemistry, Medicinal
Anish Parmar, Rajamani Lakshminarayanan, Abhishek Iyer, Eunice Tze Leng Goh, Tsz Ying To, Joey Kuok Hoong Yam, Liang Yang, Enas Newire, Maria C. Robertson, Stephen H. Prior, Eefjan Breukink, Annemieke Madder, Ishwar Singh
Summary: Teixobactin analogues with simplified structures, consisting of commercially available hydrophobic amino acid residues and various combinations of arginines, showed potent antibacterial activity against a broad range of Gram-positive bacteria, including MRSA and VRE strains. These analogues also demonstrated strong antibiofilm activity against Staphylococcus species associated with chronic infections, providing insights for the synthesis of highly potent Teixobactin analogues to combat resistant bacterial infections and biofilms.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Engineering, Biomedical
Xinshu Zou, Shuang Cai, Tingting Wang, Sidi Zheng, Xilong Cui, Jingyou Hao, Xueying Chen, Yanyan Liu, Zhiyun Zhang, Yanhua Li
Summary: In this study, pH-responsive nanoparticles were developed to effectively eliminate intracellular MRSA infection. These nanoparticles can specifically target infected macrophages/MRSA and release natural antibacterial agents to kill the bacteria. The strategy effectively eradicated intracellular MRSA by downregulating bacterial toxins, decreasing cell damage, and reducing bacterial dissemination risk. This approach presents a potential alternative for enhancing intracellular MRSA therapy.
ACTA BIOMATERIALIA
(2023)
Article
Nanoscience & Nanotechnology
Ning Li, He-Kuan Luo, Adrielle Xianwen Chen, Jeremy Pang Kern Tan, Chuan Yang, Melgious Jin Yan Ang, Huaqiang Zeng, Yi Yan Yang
Summary: This study introduces a novel class of supramolecules with highly potent antimicrobial activities. These supramolecules exhibit high antimicrobial potency against various bacteria and fungus, with negligible toxicity to mammalian cells.
ACS APPLIED MATERIALS & INTERFACES
(2022)
Article
Chemistry, Multidisciplinary
Lu Jiang, Pei Lin Chee, Jian Gao, Ching Ruey Raymond Gan, Cally Owh, Rajamani Lakshminarayanan, Shan Jiang, T. S. Andy Hor, Xian Jun Loh
Summary: The study revealed that the bis-methylphenyl-substituted porphyrins have superior bactericidal activities with low hemotoxicity and good cytotoxicity profile, even in the dark.
CHEMISTRY-AN ASIAN JOURNAL
(2021)
Article
Chemistry, Medicinal
Raj K. C. Hansa, M. M. K. Khan, M. M. Frangie, D. F. Gilmore, R. S. Shelton, A. Savenka, A. G. Basnakian, S. L. Shuttleworth, M. S. Smeltzer, M. A. Alam
Summary: A collection of potent antimicrobials has been synthesized and tested for antibacterial activity, showing low toxicity to human cells. Two compounds were highly effective against Staphylococcus aureus, with a low tendency for resistance development. In vivo mouse studies showed no harmful effects at doses up to 50 mg/kg.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Diana Pereira, Tiago Soares Carreira, Nuno Alves, Angela Sousa, Joana F. A. Valente
Summary: The global COVID-19 pandemic has raised awareness of the risk posed by microorganisms to human well-being and survival. Scientists worldwide are actively searching for solutions to kill or slow down the spread of the virus. Metals have been extensively studied as antimicrobial solutions.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Infectious Diseases
Kenneth Sue, Melissa M. Cadelis, Thomas Troia, Florent Rouvier, Marie-Lise Bourguet-Kondracki, Jean Michel Brunel, Brent R. Copp
Summary: With the rise of antibiotic resistance, the search for new antibacterial agents is becoming increasingly important. The discovery of squalamine in 1993 has sparked interest in the study of simplified cholic acid-polyamine derivatives. This study focuses on the synthesis of deoxycholic acid-polyamine conjugates and identifies hyodeoxycholic acid derivatives as potent against S. aureus MRSA and certain fungal strains, without any cytotoxicity or hemolytic properties. Further investigation reveals that analogue 7e exhibits bactericidal activity against Gram-positive bacteria, and its mechanism of action does not involve the bacterial membrane as a primary cellular target.
Article
Chemistry, Medicinal
Jing Xia, Yun Li, Cailu He, Can Yong, Li Wang, Huan Fu, Xiao-Long He, Zhou-Yu Wang, Dong-Fang Liu, Yuan-Yuan Zhang
Summary: A series of pleuromutilin derivatives containing an oxazolidinone skeleton showed potent antibacterial activities against Staphylococcus aureus and Staphylococcus epidermidis. Compound 28 exhibited the most active antibacterial activity in vitro.
ACS INFECTIOUS DISEASES
(2023)
Article
Chemistry, Medicinal
Satyaveni Malasala, Md Naiyaz Ahmad, Ravikumar Akunuri, Manjulika Shukla, Grace Kaul, Arunava Dasgupta, Y. Madhavi, Sidharth Chopra, Srinivas Nanduri
Summary: Fifteen new Quinazoline-benzimidazole hybrids were designed and synthesized, leading to the identification of nine potent antibacterial agents with activity against drug-resistant S. aureus. These compounds showed low toxicity to Vero cells and promising selectivity index, indicating their potential as antimicrobial agents for MDR-S. aureus and Mycobacterial infections.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Engineering, Biomedical
Ziyi Lu, Yueming Wu, Zihao Cong, Yuxin Qian, Xue Wu, Ning Shao, Zhongqian Qiao, Haodong Zhang, Yunrui She, Kang Chen, Hengxue Xiang, Bin Sun, Qian Yu, Yuan Yuan, Haodong Lin, Meifang Zhu, Runhui Liu
Summary: The peptide polymer-modified thermoplastic polyurethane (TPU) surfaces exhibit broad-spectrum antibacterial properties and good biocompatibility, functioning through a contact-killing mechanism by disrupting the bacterial membrane.
BIOACTIVE MATERIALS
(2021)
Article
Infectious Diseases
Junshu Yang, Christopher Brown, Wayland Noland, Timothy J. Johnson, Yinduo Ji
Summary: The slow discovery of new antibiotics and the rapid development of bacterial resistance have put us in a vulnerable position. We are running out of effective treatment options for antibiotic-resistant infections. However, a study has identified a promising molecule called MZ-01, which exhibits potent bactericidal activity against multidrug-resistant Gram-positive bacterial pathogens, including MRSA. MZ-01 also has low cytotoxicity, making it a potential scaffold for the development of novel antibacterial agents.
Article
Cell Biology
Craig Fenwick, Priscilla Turelli, Laurent Perez, Celine Pellaton, Line Esteves-Leuenberger, Alex Farina, Jeremy Campos, Erica Lana, Flurin Fiscalini, Charlene Raclot, Florence Pojer, Kelvin Lau, Davide Demurtas, Marc Descatoire, Victor S. Joo, Mathilde Foglierini, Alessandra Noto, Rana Abdelnabi, Caroline S. Foo, Laura Vangeel, Johan Neyts, Wenjuan Du, Berend-Jan Bosch, Geertruida Veldman, Pieter Leyssen, Volker Thiel, Roger LeGrand, Yves Levy, Didier Trono, Giuseppe Pantaleo
Summary: The research has identified a monoclonal antibody called P5C3 with highly potent neutralizing activity against all SARS-CoV-2 variants identified to date, showing promising potential as a prophylactic agent or combination therapy for individuals with poor response to vaccination.
Article
Microbiology
Pengfei She, Yifan Yang, Linhui Li, Yimin Li, Shasha Liu, Zehao Li, Linying Zhou, Yong Wu
Summary: This study found that the antimalarial agent TAF showed antimicrobial efficacy against methicillin-resistant Staphylococcus aureus (MRSA) and its highly resistant phenotypes of biofilm and persister cells. TAF exerted its antimicrobial activity mainly through selective bacterial cell membrane disruption. It also exhibited effective antimicrobial effect in an animal model of subcutaneous abscess. These findings suggest that TAF has the potential to be developed as a new antimicrobial agent to treat refractory MRSA infections.
Article
Chemistry, Physical
Zhen Li, Rosario Nunez, Mark E. Light, Eliseo Ruiz, Francesc Teixidor, Clara Vinas, Daniel Ruiz-Molina, Claudio Roscini, Jose Giner Planas
Summary: In this study, we design and synthesize a series of water-stable and temperature-stable mCB-EuyTb1-y MOFs and report the tunable emission, energy transfer, and time-dependent emission of these materials. The quantum yield is significantly increased and the lifetime luminescence is enhanced and tunable, achieved by a highly effective energy transfer process. The time-dependent emission and high quantum yield provide a simple method for designing high-security anticounterfeiting materials.
CHEMISTRY OF MATERIALS
(2022)
Article
Multidisciplinary Sciences
Jordi Poater, Clara Vinas, Miquel Sola, Francesc Teixidor
Summary: This study investigates the possibility of 3D/2D aromatic fusions and their relationship to electronic delocalization. While 2D/2D and 3D/3D aromatic fusions have been synthesized, the ineffective overlap between the pi-MOs of planar species and the n + 1 molecular orbitals in the aromatic cage makes 3D/2D aromatic combination impossible.
NATURE COMMUNICATIONS
(2022)
Article
Oncology
Annette G. Beck-Sickinger, Daniel P. Becker, Oksana Chepurna, Bhaskar Das, Sebastian Flieger, Evamarie Hey-Hawkins, Narayan Hosmane, Satish S. Jalisatgi, Hiroyuki Nakamura, Rameshwar Patil, Maria da Graca H. Vicente, Clara Vinas
Summary: This article summarizes current research on the development of boron delivery drugs for boron neutron capture therapy, which were presented and discussed at the National Cancer Institute (NCI) Workshop on Neutron Capture Therapy held on April 20-22, 2022. The most commonly used boron sources are icosahedral boron clusters attached to various molecules such as peptides, proteins, porphyrin derivatives, dendrimers, polymers, and nanoparticles, as well as encapsulated into liposomes. These boron clusters and/or carriers can be labeled with contrast agents, allowing for imaging techniques like PET, SPECT, and fluorescence to quantify tumor-localized boron and serve as theranostic agents.
CANCER BIOTHERAPY AND RADIOPHARMACEUTICALS
(2023)
Article
Chemistry, Organic
Mingyan Ding, Jonathan A. Reuven, Andrew C. Hones, Mark A. Fox, Patrick G. Steel
Summary: The iridium catalysed C-H borylation of polyfluorinated arenes and heteroarenes occurs rapidly and efficiently. Steric parameters dominate the borylation reactions, but there is also an underlying electronic influence on reaction selectivity. The regioselectivity of borylation in fluorinated (hetero)arenes is mainly determined by electronic effects, except for ortho-borylation between two fluorine atoms where steric effects become apparent. Good agreement between predicted and observed selectivities is achieved by considering transition state energies in iridium geometries.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Article
Chemistry, Inorganic & Nuclear
Ross Davidson, Yu-Ting Hsu, Mark A. Fox, Juan A. Aguilar, Dmitry Yufit, Andrew Beeby
Summary: This study investigates the emission behavior of Ir(ppy)2(acac) complexes with OPE3 motifs and finds that the complexes containing OPE3 structures have long emission lifetimes, which can be achieved through intramolecular reversible electronic energy transfer (REET) with even longer-lived localized OPE3 states. This finding is important for oxygen sensing and cellular imaging applications.
INORGANIC CHEMISTRY
(2023)
Review
Biochemistry & Molecular Biology
Anca-Iulia Stoica, Clara Vinas, Francesc Teixidor
Summary: This work highlights the applications of the theta metallabis(dicarbollide) cluster in preparing sensors for monitoring amine-containing drugs or other nitrogen-containing molecules. The developed electrodes show Nernstian responses for target analytes, such as antibiotics, amino acids, neurotransmitters, and analgesics.
Article
Chemistry, Multidisciplinary
Jessica L. Andrews, Dmitry S. Yufit, James F. McCabe, Mark A. Fox, Jonathan W. Steed
Summary: This example demonstrates that vapor sorption is a potentially valuable yet underutilized tool for modifying pharmaceutical solid forms as part of a solid form screening protocol.
CRYSTAL GROWTH & DESIGN
(2023)
Article
Chemistry, Inorganic & Nuclear
Ahmed M'hamedi, Andrei S. Batsanov, Mark A. Fox, Juan A. Aguilar, Martin R. Bryce
Summary: Six new diiridium complexes with 2-methyl-6-phenylpyridyl as the cyclometalating ligand and mu(2)-oxamidato or mu(2)-dithioxamidato as the bridging ligand have been synthesized. The presence of multiple isomers in these complexes was confirmed by NMR and X-ray crystallography, and computational calculations supported the experimental findings. The emission spectra of these complexes were attributed to mixed metal-ligand to ligand charge transfer excited states.
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Ricardo G. Teixeira, Janos P. Meszaros, Beatriz Matos, Leonor Corte-Real, Cristina P. R. Xavier, Xavier Fontrodona, M. Helena Garcia, Isabel Romero, Gabriella Spengler, M. Helena Vasconcelos, Ana Isabel Tomaz, Eva A. Enyedy, Andreia Valente
Summary: This article presents the synthesis and properties of a series of novel ruthenium(II)-cyclopentadienyl organometallic compounds. These compounds exhibit high activity in anti-cancer and antibacterial applications. Compounds 6 and 7 show remarkable inhibitory effects on colorectal cancer and non-small cell lung cancer. Additionally, these compounds demonstrate potent antibacterial activity against methicillin-resistant Staphylococcus aureus strains. The study also reveals interactions between these complexes and human serum albumin and calf thymus DNA.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Leonor Corte-Real, Vivien Posa, Matilde Martins, Raquel Colucas, Nora V. May, Xavier Fontrodona, Isabel Romero, Filipa Mendes, Catarina Pinto Reis, Maria Manuela Gaspar, Joao Costa Pessoa, Eva A. Enyedy, Isabel Correia
Summary: In this study, three novel Schiffbases (L1-L3) derived from the condensation of 2-carbaldehyde-8-hydroxyquinoline with amines containing morpholine or piperidine moieties were synthesized and characterized. These Schiffbases were reacted with CuCl2 and ZnCl(2) to yield six new coordination compounds, which were all characterized using various techniques. The Cu(II) complexes showed higher stability and anticancer activity than the Zn(II) complexes.
INORGANIC CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Enric Clerich, Syrine Affes, Enriqueta Antico, Xavier Fontrodona, Francesc Teixidor, Isabel Romero
Summary: A new bidentate pyridylpyrazole ligand functionalized with the pyrene group was synthesized, and its homogeneous photoredox catalyst with the tridentate terpyridine was investigated. The molecular complexes were heterogenized on reduced graphene oxide through noncovalent interactions and used in the photooxidation reactions of alcohols and trans-beta-methylstyrene. The results showed improved yields and good recyclability due to the presence of the pyrene group and its anchoring to the graphene support.
INORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Chemistry, Inorganic & Nuclear
Ines Bennour, M. Nuria Ramos, Miquel Nuez-Martinez, Jewel Ann Maria Xavier, Ana B. Buades, Reijo Sillanpaa, Francesc Teixidor, Duane Choquesillo-Lazarte, Isabel Romero, Margarita Martinez-Medina, Clara Vinas
Summary: In this study, the synthesis and characterization of two small molecules were reported. One of the compounds showed antimicrobial activity against Candida species and Gram-positive/negative bacteria with low toxicity, making it a potential candidate for antimicrobial therapy. Moreover, the influence of compound structure and environmental factors on antimicrobial properties was investigated.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Pedro O. Abate, Analia M. Peyrot, Xavier Fontrodona, Isabel Romero, Florencia Fagalde, Nestor E. Katz
Summary: New ruthenium polypyridyl complexes were synthesized and characterized, showing potential applications in detecting acetonitrile contaminants and catalyzing water oxidation processes.