0000000000436045

AUTHOR

Clementina Cocuzza

showing 5 related works from this author

New linezolid-like 1,2,4-oxadiazoles active against Gram-positive multiresistant pathogens

2013

The synthesis and the in vitro antibacterial activity of novel linezolid-like oxadiazoles are reported. Replacement of the linezolid morpholine C-ring with 1,2,4-oxadiazole results in an antibacterial activity against Staphylococcus aureus both methicillin-susceptible and methicillin-resistant comparable or even superior to that of linezolid. While acetamidomethyl or thioacetoamidomethyl moieties in the C(5) side-chain are required, fluorination of the phenyl B ring exhibits a slight effect on an antibacterial activity but its presence seems to reduce the compounds cytotoxicity. Molecular modeling performed using two different approaches - FLAP and Amber software - shows that in the binding…

Methicillin-Resistant Staphylococcus aureusModels MolecularCell viabilityStaphylococcus aureusMolecular modelCell SurvivalMicrobial Sensitivity TestsAntimicrobial activityCrystallography X-Raymedicine.disease_causeDrug designMicrobiologyStructure-Activity Relationshipchemistry.chemical_compoundoxadiazoles linezolid antibioticsCell Line TumorDrug Resistance Multiple BacterialMorpholineAcetamidesDrug DiscoverymedicineHumansMoietyStructure–activity relationshipOxazolidinonesPharmacologyOxadiazolesOxazolidinones; Linezolid; Drug designDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistryLinezolidSettore CHIM/06 - Chimica OrganicaHep G2 CellsGeneral Medicinebiochemical phenomena metabolism and nutritionbacterial infections and mycosesSettore CHIM/08 - Chimica FarmaceuticaMethicillin-resistant Staphylococcus aureusCombinatorial chemistryOxazolidinoneAnti-Bacterial AgentsStaphylococcus aureusMED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICALinezolidAntimicrobial activity; Cell viability; Drug design; Oxazolidinones; Staphylococcus aureusAntibacterial activitySoftware
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New potent antibacterials against Gram-positive multiresistant pathogens: effects of side chain modification and chirality in linezolid-like 1,2,4-ox…

2014

The effects of side chain modification and chirality in linezolid-like 1,2,4-oxadiazoles have been studied to design new potent antibacterials against Gram-positive multidrug-resistant pathogens. The adopted strategy involved a molecular modelling approach, the synthesis and biological evaluation of new designed compounds, enantiomers separation and absolute configuration assignment. Experimental determination of the antibacterial activity of the designed (S)-1-((3-(4-(3-methyl-1,2,4-oxadiazol-5- yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea and (S)-1-((3-(3-fluoro-4-(3-methyl-1,2,4- oxadiazol-5-yl)phenyl)-oxazolidin-2-one-5-yl)methyl)-3-methylthiourea against multidrug resistan…

Multidrug-resistant bacteriaClinical BiochemistryAntibioticsDrug ResistanceMolecular ConformationPharmaceutical ScienceBiochemistrychemistry.chemical_compoundAntibioticsDrug Resistance Multiple BacterialDrug DiscoveryAcetamidesSide chainOxadiazolesAbsolute configurationBacterialStereoisomerismHep G2 CellsBIO/10 - BIOCHIMICA23SAnti-Bacterial AgentsMolecular Docking SimulationRNA Ribosomal 23SDrug design Linezolid Antibiotics Multidrug-resistant bacteria EnantiomersMolecular MedicineAntibacterial activityMultipleMethicillin-Resistant Staphylococcus aureusStaphylococcus aureusmedicine.drug_classStereochemistryCell SurvivalMicrobial Sensitivity TestsGram-Positive BacteriaDrug designmedicineHumansMolecular BiologyOxazolidinonesRibosomalBinding SitesOrganic ChemistryAntibioticLinezolidSettore CHIM/06 - Chimica OrganicaSettore CHIM/08 - Chimica FarmaceuticaMultiple drug resistancechemistryEnantiomersMED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICALinezolidRNANucleic Acid ConformationEnantiomerChirality (chemistry)Bioorganicmedicinal chemistry
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The Effectiveness of 0.6% Povidone Iodine Eye Drops in Reducing the Conjunctival Bacterial Load and Needle Contamination in Patients Undergoing Anti-…

2019

The study purpose was to assess the efficacy of a preservative-free 0.6% povidone iodine eye drops as perioperative prophylactic treatment for reducing conjunctival bacterial load and the rate of needle contamination in patients undergoing intravitreal anti-vascular endothelial growth factor injection. Enrolled patients were randomized to either the study group (0.6% povidone iodine, three day-prophylactic treatment before the injection) or to the control group (placebo, three day-prophylactic treatment). Conjunctival swabs were obtained before and after the prophylactic treatment in both groups. Intravitreal injections were performed in a sterile fashion. The injection needle and a control…

Microbiological culturechemistry.chemical_elementlcsh:Medicineconjunctival flora; endophthalmitis; intravitreal injection; needle contamination; povidone iodinePlaceboIodineArticle03 medical and health sciencesconjunctival flora0302 clinical medicineEndophthalmitisneedle contamination0502 economics and businessMedicineIn patientAdverse effectpovidone iodinebusiness.industry05 social scienceslcsh:Rintravitreal injectionGeneral MedicinePerioperativeContaminationmedicine.diseaseendophthalmitichemistryendophthalmitisAnesthesia030221 ophthalmology & optometry050211 marketingbusinessJournal of Clinical Medicine
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Wastewater surveillance of SARS-CoV-2 variants in October-November 2022 in Italy: detection of XBB.1, BA.2.75 and rapid spread of the BQ.1 lineage

2023

This study adds insight regarding the occurrence and spread of SARS-CoV-2 Variants of Concern (VOCs) and Var-iants of Interest (VOIs) in Italy in October and November 2022, by testing urban wastewater collected through-out the country. A total of 332 wastewater samples were collected from 20 Italian Regions/Autonomous Provinces (APs) within the framework of national SARS-CoV-2 environmental surveillance. Of these, 164 were collected in the first week of October and 168 in the first week of November. A similar to 1600 bp fragment of the spike protein was sequenced by Sanger (for individual samples) and long-read nanopore sequencing (for pooled Region/AP samples).In October, mutations charact…

BA2.75Environmental EngineeringSurveillanceMED/42 - IGIENE GENERALE E APPLICATAOmicronSARS-CoV-2BQ.1BA2.75; BQ.1; Omicron; SARS-CoV-2; Surveillance; Wastewater; XBB.1WastewaterBIO/19 - MICROBIOLOGIA GENERALEPollutionMED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICABA2.75 BQ.1 Omicron SARS-CoV-2 Surveillance Wastewater XBB.1XBB.1Environmental ChemistryWaste Management and Disposal
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Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives

2012

In the present study the synthesis of new Linezolid-like molecules has been achieved by substitution of the oxazolidinone central heterocyclic moiety with a 1,2,4-oxadiazole ring. Two series of 1,2,4-oxadiazoles, bearing different side-chains and containing a varying number of fluorine atoms, were synthesized and preliminarily tested for biological activity against some Gram-positive and Gram-negative bacteria using Linezolid and Ceftriaxone as reference drugs

StereochemistryOxadiazoleMicrobial Sensitivity TestsAntimicrobial activityRing (chemistry)Oxazolidinone 124-Oxadiazole Linezolid Antimicrobial activity Fluorinated heterocyclesStructure-Activity Relationshipchemistry.chemical_compoundFluorinated heterocyclesAcetamidesDrug DiscoveryMoleculeMoiety124-OxadiazoleOxazolidinonesPharmacologyBacteriaMolecular StructureCeftriaxoneOrganic ChemistryLinezolidBiological activitySettore CHIM/06 - Chimica OrganicaGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaOxazolidinoneAnti-Bacterial AgentschemistryMED/07 - MICROBIOLOGIA E MICROBIOLOGIA CLINICALinezolid
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