6533b872fe1ef96bd12d42b2

RESEARCH PRODUCT

New Thiazole Nortopsentin Analogues Inhibit Bacterial Biofilm Formation.

Girolamo CirrincioneMaria Grazia CusimanoCascioferro StellaAlessandra MontalbanoPaola BarrajaAnna CarboneDomenico SchillaciPatrizia DianaVirginia SpanòBarbara Parrino

subject

0301 basic medicinethiazole derivativeAquatic OrganismsIndolesDrug ResistancePharmaceutical ScienceBacterial growthAntibiofilm agentmedicine.disease_cause01 natural scienceschemistry.chemical_compoundDrug Discoveryanti-virulence agents; antibiofilm agents; marine alkaloids; nortopsentin analogues; thiazole derivatives; Anti-Bacterial Agents; Aquatic Organisms; Biofilms; Humans; Imidazoles; Indoles; Inhibitory Concentration 50; Staphylococcal Infections; Staphylococcus aureus; Thiazoles; Drug Resistance; Bacterial; Anti-virulence agents; Antibiofilm agents; Marine alkaloids; Nortopsentin analogues; Thiazole derivativesPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Aquatic OrganismBiofilmBacterialImidazolesantibiofilm agentsStaphylococcal InfectionsAnti-Bacterial Agentsnortopsentin analoguesBiochemistryStaphylococcus aureusStaphylococcus aureumarine alkaloidsthiazole derivativesSelectivityHumanStaphylococcus aureusAnti-virulence agentNortopsentin analogueArticle03 medical and health sciencesInhibitory Concentration 50Anti-Bacterial AgentDrug Resistance BacterialIc50 valuesmedicineHumansThiazoleImidazoleStaphylococcal Infection010405 organic chemistryBiofilmSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesmarine alkaloidThiazoles030104 developmental biologychemistrylcsh:Biology (General)anti-virulence agentsIndoleBiofilmsThiazole

description

New thiazole nortopsentin analogues were conveniently synthesized and evaluated for their activity as inhibitors of biofilm formation of relevant Gram-positive and Gram-negative pathogens. All compounds were able to interfere with the first step of biofilm formation in a dose-dependent manner, showing a selectivity against the staphylococcal strains. The most active derivatives elicited IC50 values against Staphylococcus aureus ATCC 25923, ranging from 0.40&ndash

10.3390/md16080274https://pubmed.ncbi.nlm.nih.gov/30081568