Search results for "anti-biofilm agent"

showing 6 items of 6 documents

Synthetic small molecules as anti-biofilm agents in the struggle against antibiotic resistance

2018

Abstract Biofilm formation significantly contributes to microbial survival in hostile environments and it is currently considered a key virulence factor for pathogens responsible for serious chronic infections. In the last decade many efforts have been made to identify new agents able to modulate bacterial biofilm life cycle, and many compounds have shown interesting activities in inhibiting biofilm formation or in dispersing pre-formed biofilms. However, only a few of these compounds were tested using in vivo models for their clinical significance. Contrary to conventional antibiotics, most of the anti-biofilm compounds act as anti-virulence agents as they do not affect bacterial growth. I…

Antibiotic resistancemedicine.drug_classAntibioticsMicrobial Sensitivity TestsBacterial growthDispersal agent01 natural sciencesVirulence factorMicrobiologySmall Molecule LibrariesStructure-Activity Relationship03 medical and health sciencesAntibiotic resistanceSmall Molecule LibrarieAnti-Bacterial AgentDrug Discoverymedicine030304 developmental biologyPharmacology0303 health sciencesBacteriaDose-Response Relationship DrugMolecular StructureMicrobial Sensitivity Test010405 organic chemistryChemistryBiofilmOrganic ChemistryBiofilmDrug Resistance MicrobialGeneral Medicinebiochemical phenomena metabolism and nutritionAnti-biofilm agentSettore CHIM/08 - Chimica FarmaceuticaSmall moleculeAnti-Bacterial Agents0104 chemical sciencesAnti-adhesion agentBiofilmsAnti-virulence compoundAnti biofilmEuropean Journal of Medicinal Chemistry
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2,6-Disubstituted imidazo[2,1-b][1,3,4]thiadiazole derivatives as potent staphylococcal biofilm inhibitors.

2019

Abstract A class of 36 new 2-(6-phenylimidazo[2,-1-b][1,3,4]thiadiazol-2-yl)-1H-indoles was efficiently synthesized and evaluated for their anti-biofilm properties against the Gram-positive bacterial reference strains Staphylococcus aureus ATCC 25923, S. aureus ATCC 6538 and Staphylococcus epidermidis ATCC 12228, and the Gram-negative strains Pseudomonas aeruginosa ATCC 15442 and Escherichia coli ATCC 25922. Many of these new compounds, were able to inhibit biofilm formation of the tested staphylococcal strains showing BIC50 lower than 10 μg/ml. In particular, derivatives 9c and 9h showed remarkable anti-biofilm activity against S. aureus ATCC 25923 with BIC50 values of 0.5 and 0.8 μg/ml, r…

Indoles3Anti-virulence agentStaphylococcus1-b][1Bacterial growthAnti-Biofilm agentsmedicine.disease_causeSettore BIO/19 - Microbiologia GeneraleGram-Positive Bacteriaimidazo[201 natural sciencesVirulence factorMicrobiology03 medical and health sciencesStaphylococcus epidermidisDrug DiscoveryGram-Negative BacteriaThiadiazolesmedicineStaphylococcal biofilm inhibitorsEscherichia coli030304 developmental biologyPharmacology0303 health sciences4]thiadiazole derivativesbiologyStaphylococcal biofilm inhibitorVirulenceAnti-Biofilm agents; Anti-virulence agents; imidazo[21-b][134]thiadiazole derivatives; Staphylococcal biofilm inhibitors; Anti-Bacterial Agents; Biofilms; Gram-Negative Bacteria; Gram-Positive Bacteria; Indoles; Staphylococcus; Thiadiazoles; Virulence010405 organic chemistryPseudomonas aeruginosaChemistryimidazo[21-b][134]thiadiazole derivativesOrganic ChemistryBiofilmGeneral Medicinebiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticaAnti-Biofilm agent0104 chemical sciencesAnti-Bacterial AgentsAnti-virulence agentsStaphylococcus aureusBiofilms1 3 4 thiadiazole derivativesEuropean journal of medicinal chemistry
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Development of natural and synthetic compounds as kinase inhibitors targeting cancer cells and cancer stem cells

2023

Pancreatic ductal adenocarcinomaInhibition of migrationantibiotic resistanceImidazo[21-b][134]thiadiazole derivativeskinase inhibitorsanti-biofilm agentsAntiproliferative activityFAK inhibitionSettore CHIM/08 - Chimica Farmaceutica
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Inhibitors of antibiotic resistance mechanisms: clinical applications and future perspectives

2020

Bacterial strains responsible for antibiotic resistant infections are increasing in an alarming way and the evolution of resistance mechanisms seems to be unstoppable. In the past decade, many efforts have been made in order to counteract this phenomenon but very few compounds have reached clinical trials. The development of new classes of antibiotics able to overcome the main bacterial drug resistance mechanisms is urgently required to counter the imminent danger of a postantibiotic era.

Pharmacologymedicine.medical_specialtyantibiotic resistanceBacteriaChemistryantivirulence strategyDrug Resistance MicrobialMicrobial Sensitivity TestsAnti-Bacterial Agentsanti-biofilm agentAntibiotic resistanceDrug DiscoveryESKAPE pathogensmedicineMolecular MedicineIntensive care medicine
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Pyrrolomycins as potential anti-staphylococcal biofilms agents

2010

With the goal of discovering new anti-infective agents active against microbial biofilms, this investigation focused on some natural pyrrolomycins, a family of halogenated pyrrole antibiotics. In this study the anti-staphylococcal biofilm activity of pyrrolomycins C, D, F1, F2a, F2b, F3 and of the synthesized related compounds I, II, III were investigated. The susceptibility of six staphylococcal biofilms was determined by methyltiazotetrazolium staining. Most of the compounds were active at concentrations of 1.5 microg ml(-1) with significant inhibition percentages. A few of the compounds were active at the lowest screening concentration of 0.045 microg ml(-1). The population log reduction…

Staphylococcus aureusSynthetic derivativesmedicine.drug_classCell SurvivalAntibioticsPopulationMicrobial Sensitivity TestsAquatic ScienceBiologymedicine.disease_causeSettore BIO/19 - Microbiologia GeneraleApplied Microbiology and BiotechnologyPolymerase Chain ReactionBacterial AdhesionMicrobiologyCell LineInhibitory Concentration 50medicineStaphylococcus epidermidisHumansPyrroleseducationWater Science and TechnologyMicrobial BiofilmsCell Proliferationeducation.field_of_studyMolecular StructureBiofilmStainingAnti-Bacterial AgentsStaphylococcal biofilms Anti-biofilm agents PyrrolomycinsStaphylococcus aureusBiofilmsToxicity
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Synthesis and biological evaluation of new imidazo[2,1-b][1,3,4]thiadiazole derivatives: as anticancer and antibiofilm agents, and preclinical invest…

2020

antiproliferative activityStaphylococcal biofilm inhibitorhypoxiaAnti-virulence agentpancreatic ductal adenocarcinomachemoresistancemodulation of EMTlactate dehydrogenaseproton-coupled folate transporterspheroids shrinkageSettore CHIM/08 - Chimica Farmaceuticamalignant pleural and peritoneal mesotheliomaanti-biofilm agentimidazo[21-b][134]thiadiazole derivativeinhibition of migrationPTK2/FAKxenograftpemetrexedprognosi
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