Targeting bacterial efflux pump effectively enhances the efficacy of Ru-based antibacterial agents against Gram-negative pathogen.

The rise of antibiotic resistance has posed a great threat to human's life, thus develop novel antibacterial agents is urgently needed. It worthies to noted that Ru-based antibacterial agents often showed robust potency against Gram-positive pathogens, disrupted bacterial membrane and avoided bacterial resistance, making they promising antibiotic candidates. However, they are generally less active when applied to negative pathogens.

AIE-based ruthenium complexes as photosensitizers for specifically photo-inactivate gram-positive bacteria.

The emergence of multidrug-resistant bacterial have caused severe burden for public health. Particularly, Staphylococcus aureus as one of ESKAPE pathogens have induced various infectious diseases and resulted in increasing deaths. Developing new antibacterial agents is still urgent and challenging.

Discovery of quaternized pyridine-thiazole-ruthenium complexes as potent anti-Staphylococcus aureus agents.

Quaternization of ruthenium complexes may be a promising strategy for the development of new antibiotics. In response to the increasing bacterial resistance, we integrated the quaternary amine structure into the design of ruthenium complexes and evaluated their antibacterial activity. All the ruthenium complexes showed good antibacterial activity against the tested Staphylococcus aureus (S.

Enabling Modular Click Chemistry Library through Sequential Ligations of Carboxylic Acids and Amines.

High-throughput synthesis and screening of chemical libraries play pivotal roles in drug discovery. Click chemistry has emerged as a powerful strategy for constructing highly modular chemical libraries. However, the development of new click reactions and unlocking new clickable building blocks remain exceedingly challenging.

Design, synthesis, anti-infective potency and mechanism study of novel Ru-based complexes containing substituted adamantane as antibacterial agents.

Infections caused by Staphylococcus aureus (S. aureus) are increasing difficult to treat because this pathogen is easily resistant to antibiotics. However, the development of novel antibacterial agents with high antimicrobial activity and low frequency of resistance remains a huge challenge.

Polypyridyl ruthenium complexes with benzothiazole moiety as membrane disruptors and anti-resistance agents for Staphylococcus aureus.

Developing new antimicrobials to combat drug-resistant bacterial infections is necessary due to the increasing problem of bacterial resistance. In this study, four metallic ruthenium complexes modified with benzothiazoles were designed, synthesized and subjected to bio-evaluated. Among them, Ru-2 displayed remarkable inhibitory activity against Staphylococcus aureus (S.

Metal-ruthenium complex based on dipyridylamine group as membrane-active antibacterial agent effectively decrease the development of drug-resistance on Staphylococcus aureus.

Staphylococcus aureus (S. aureus), one of the Gram-positive bacteria, is easily to develop drug-resistance. Drug-resistant S.

Coupling a Virulence-Targeting Moiety with Ru-Based AMP Mimics Efficiently Improved Its Anti-Infective Potency and Therapeutic Index.

The surge of antibiotic resistance in calls for novel drugs that attack new targets. Developing antimicrobial peptides (AMPs) or antivirulence agents (AvAs) is a promising strategy to tackle this challenge. However, AMPs, which kill bacteria by disrupting cell membranes, suffer from low stability and high synthesis cost, while AvAs, which inhibit toxin secretion, have relatively poor bactericidal activity.

Ruthenium polypyridine complexes containing prenyl groups as antibacterial agents against Staphylococcus aureus through a membrane-disruption mechanism.

Four new ruthenium polypyridyl complexes with prenyl groups, [Ru(bpy) (MHIP)](PF ) (Ru(II)-1), [Ru(dtb) (MHIP)](PF ) (Ru(II)-2), [Ru(dmb) (MHIP)](PF ) (Ru(II)-3), and [Ru(dmob) (MHIP)](PF ) (Ru(II)-4) (bpy = 2,2'-bipyridine, dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dmob = 4,4'-dimethoxy-2,2'-bipyridine, and MHIP = 2-(2,6-dimethylhepta-1,5-dien-1-yl)-1H-imidazo[4,f][1,10]phenanthroline), were synthesized and characterized. Their antibacterial activities against Staphylococcus aureus were assessed, and the minimum inhibition concentration (MIC) value of Ru(II)-2 against S. aureus was only 0.

Coumarin-modified ruthenium complexes by disrupting bacterial membrane to combat Gram-positive bacterial infection.

Antibiotic abuse has caused the generation of drug-resistant bacteria and a series of infections induced by multidrug-resistant bacteria have become a threat to human health. Facing the failure of traditional antibiotics, antibacterial drugs with new molecular and action modes urgently need to be developed. In this study, ruthenium complexes containing coumarin were designed and synthesized.

Synthesis and biological evaluation of ruthenium complexes bearing the 1,2,4-triazole group as potential membrane-targeting antibacterial agents towards .

Bacterial infection is one of the most serious public health problems, being harmful to human health and expensive. Nowadays, the misuse and overuse of antibiotics have led to the emergence of drug resistance. Therefore, it is an urgent need to develop new antimicrobial agents to address the current situation.

Multi-target antibacterial mechanism of ruthenium polypyridine complexes with anthraquinone groups against .

Three new Ru(ii) complexes, [Ru(dtb)PPAD](PF) (), [Ru(dmob)PPAD](PF) () and [Ru(bpy)PPAD](PF) () (dtb = 4,4'-di-butyl-2,2'-bipyridine, dmob = 4,4'-dimethyl-2,2'-bipyridine, bpy = 2,2'-bipyridine and PPAD = 2-(pyridine-3-yl)-1-imidazo[4,5][1.10]phenanthracene-9,10-dione), were synthesized and characterized by H NMR and C NMR spectroscopy, HRMS and HPLC. Among them, showed excellent antimicrobial activity against Gram-positive bacteria (minimum inhibitory concentration (MIC) = 1 μg mL) and low hemolytic and cytotoxic activity.

Synthesis and biological evaluation of ruthenium complexes containing phenylseleny against Gram-positive bacterial infection by damage membrane integrity and avoid drug-resistance.

Compounds modified with selenium atom as potential antibacterial agents have been exploited to combat the nondrug-resistant bacterial infection. In this study, we designed and synthesized four ruthenium complexes retouching of selenium-ether. Fortunately, those four ruthenium complexes shown excellent antibacterial bioactive (MIC: 1.

Ruthenium polypyridine complexes with triphenylamine groups as antibacterial agents against with membrane-disruptive mechanism.

Due to the emergence and wide spread of methicillin-resistant , the treatment of this kind of infection becomes more and more difficult. To solve the problem of drug resistance, it is urgent to develop new antibiotics to avoid the most serious situation of no drug available. Three new Ru complexes [Ru (dmob)PMA] (PF6) () [Ru (bpy)PMA] (PF6) () and [Ru (dmb)PMA] (PF6) () (dmob = 4,4'-dimethoxy-2,2'-bipyridine, bpy = 2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine and PMA = N-(4-(1H-imidazo [4,5-f] [1,10] phenanthrolin-2-yl) -4-methyl-N-(p-tolyl) aniline) were synthesized and characterized by 1H NMR, 13C NMR and HRMS.

The synthesis and antibacterial activity study of ruthenium-based metallodrugs with a membrane-disruptive mechanism against .

The wide spread of drug-resistant bacteria, especially methicillin-resistant (MRSA), poses a tremendous threat to global health. Of particular concern, resistance to vancomycin, linezolid, and daptomycin has already been reported in clinical MRSA strains. New antibacterial agents are urgently needed to overcome this crisis.

Synthesis of ruthenium polypyridine complexes with benzyloxyl groups and their antibacterial activities against Staphylococcus aureus.

Four new ruthenium polypyridyl complexes, [Ru(bpy)(BPIP)](PF) (Ru(II)-1), [Ru(dtb)(BPIP)](PF) (Ru(II)-2), [Ru(dmb)(BPIP)](PF) (Ru(II)-3) and [Ru(dmob)(BPIP)](PF) (Ru(II)-4) (bpy = 2,2'-bipyridine, dtb = 4,4'-di-tert-butyl-2,2'-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dmob = 4,4'-dimethoxy-2,2'-bipyridine and BPIP = 2-(3,5-bis(benzyloxyl)phenyl)-1H-imidazo[4,5-f][1,10]phenanthroline) had been synthesized and characterized. Their antimicrobial activities were investigated against Staphylococcus aureus (S. aureus) and four complexes showed obvious antibacterial effect, especially the minimum inhibition concentration (MIC) value of Ru(II)-3 was only 4 μg/mL.

Design, synthesis, and evaluation of aryl-thioether ruthenium polypyridine complexes: A multi-target antimicrobial agents against gram-positive bacteria.

With the increase in bacterial resistance, new antimicrobial agents are urgently need for developing to combat multidrug-resistant pathogens and with low cytotoxicity. In this study, four new ruthenium polypyridine complexes bearing 4-tBu-phenyl sulfide Ru(bpy)(TBPIP)](PF)(Ru(Ⅱ)-1), Ru(dmb)(TBPIP)](PF)(Ru(Ⅱ)-2), Ru(dmob)(TBPIP)](PF)(Ru(Ⅱ)-3) and Ru(dtb)(TBPIP)](PF)(Ru(Ⅱ)-4) were designed, synthesized and evaluated. Those ruthenium complexes showed strong activity against Staphylococcus aureus (S.

Ruthenium(II) complexes targeting membrane as biofilm disruptors and resistance breakers in Staphylococcus aureus bacteria.

The development of ruthenium-based complexes or antimicrobial peptides are identified as a promising strategy for combating drug-resistant bacteria. In this work, four biphenyl-based antibacterial ruthenium complexes by targeting membrane integrity, which act as antimicrobial peptides mimics, were designed and synthesized. In vitro antimicrobial screening demonstrated that four complexes could absolutely inhibit the growth of Staphylococcus aureus (S.

Silver-mediated radical oxytrifluoromethylation of unsaturated carboxylic acids for the synthesis of γ-trifluoromethylthio lactones.

An efficient silver-mediated oxidative trifluoromethylthiolation of unsaturated carboxylic acids to construct trifluoromethylthiol-containing lactones has been disclosed. In this protocol no metal-catalysts was added, and preliminary mechanism investigations suggested that a free-radical pathway should be involved in the process. High functional group tolerance and excellent yields were demonstrated by the efficient preparation of a wide range of γ-trifluoromethylthiolated phthalides.

Synthesis and biological evaluation of ruthenium polypyridine complexes with 18β-glycyrrhetinic acid as antibacterial agents against .

Four new ruthenium(II) polypyridine complexes bearing 18β-glycyrrhetinic acid derivatives, [Ru(bpy)L](PF) (Ru1), [Ru(dmb)L](PF) (Ru2), [Ru(dtb)L](PF) (Ru3) and [Ru(phen)L](PF) (Ru4) (bpy = 2,2-bipyridine, dmb = 4,4'-dimethyl-2,2'-bipyridine, dtb = 4,4'-di--butyl-2,2'-bipyridine, phen = 1,10-phenanthroline and L is the GA modified new ligand) were designed and synthesized. Their antimicrobial activities against () were evaluated and all complexes showed an obvious inhibitory effect, especially, the minimum inhibitory concentration (MIC) value of Ru2 was 3.9 μg mL.

Synthesis of ruthenium complexes functionalized with benzothiophene and their antibacterial activity against Staphylococcus aureus.

New effective antimicrobial agents with novel modes of action are urgently needed due to the continued emergence of drug-resistant bacteria. Here, three ruthenium complexes functionalized with benzothiophene: [Ru(phen)(BTPIP)](ClO) (Ru(II)-1), [Ru(dmp)(BTPIP)](ClO) (Ru(II)-2) and [Ru(dmb)(BTPIP)](ClO) (Ru(II)-3) (dmb = 4,4'-dimethyl-2,2'-bipyridine, phen = 1,10-phenanthroline, dmp = 2,9-dimethyl-1,10-phenanthroline) have been synthesized and their antimicrobial activities in vitro were assessed. Minimum inhibitory concentration (MIC) assays indicated that the three Ru(II)-1, Ru(II)-2 and Ru(II)-3 complexes all showed antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa.

Antibacterial activity of ruthenium polypyridyl complexes against Staphylococcus aureus and biofilms.

There is clearly a need for the development of new classes of antimicrobials to fight against multidrug-resistant bacteria. Here, we designed and synthesized of three ruthenium polypyridyl complexes: [Ru(bpy)(BTPIP)](ClO) (Ru(II)-1), [Ru(bpy)(ETPIP)](ClO) (Ru(II)-2) and [Ru(bpy)(CAPIP)](ClO) (Ru(II)-3) (N-N = bpy = 2,2'-bipyridine), their antimicrobial activities against S. aureus were assessed.

Ancient events and climate adaptive capacity shaped distinct chloroplast genetic structure in the oak lineages.

Background: Understanding the origin of genetic variation is the key to predict how species will respond to future climate change. The genus Quercus is a species-rich and ecologically diverse woody genus that dominates a wide range of forests and woodland communities of the Northern Hemisphere. Quercus thus offers a unique opportunity to investigate how adaptation to environmental changes has shaped the spatial genetic structure of closely related lineages.