Search results for " Quinoxalines"

showing 4 items of 4 documents

Real-life use of elbasvir/grazoprevir in adults and elderly patients: a prospective evaluation of comedications used in the PITER cohort.

2021

Background In patients treated for HCV infection, potential drug–drug interactions (DDIs) can occur among direct-acting antiviral drugs (DAAs) and comedications used. The real-life effectiveness and safety of elbasvir/grazoprevir (ELB/GZR) among co-medicated HCV patients was evaluated. Methods We prospectively evaluated consecutive patients from 15 clinical centres participating in PITER who were treated with ELB/GZR and had been followed for at least 12 weeks after treatment. Data were prospectively collected on the use of comedications (including discontinuation, dose modification and addition of drugs) and potential DDIs with DAAs. Results Of the 356 patients with at least 12-week post-t…

Male030312 virologycombination therapytreatment experienced patientsDrug Combinationchronic hepatitis C drug drug interactions virus genotype 1 treatment experienced patients pump inhibitor use combination therapy treatment naive liver fibrosisgrazoprevir elbasvir80 and overAge FactorPharmacology (medical)Drug InteractionsProspective StudiesChronicProspective cohort studyliver fibrosisAged 80 and over0303 health sciencesAge FactorsImidazolesMiddle AgedHepatitis CDrug CombinationsInfectious DiseasesTreatment OutcomeDrug InteractionGrazoprevirCohortdrug drug interactionsFemalepump inhibitor useHumanmedicine.drugmedicine.medical_specialtyElbasvirQuinoxalinetreatment naiveelbasvirAntiviral AgentsNO03 medical and health sciencesInternal medicineQuinoxalinesmedicinechronic hepatitis CElbasvir GrazoprevirHumansImidazoleAgedBenzofuransAntiviral AgentPharmacology...business.industrygrazoprevirCarbamazepineHepatitis C Chronicmedicine.diseaseComorbidityDiscontinuationBenzofuranAge Factors; Aged; Aged 80 and over; Antiviral Agents; Benzofurans; Drug Combinations; Drug Interactions; Female; Hepatitis C Chronic; Humans; Imidazoles; Male; Middle Aged; Prospective Studies; Quinoxalines; Treatment Outcomebusinessvirus genotype 1Antiviral therapy
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Aza-isoindolo and isoindolo-azaquinoxaline derivatives with antiproliferative activity

2015

Abstract Three new ring systems, pyrido[2′,3′:3,4]pyrrolo[1,2- a ]quinoxalines, pyrido[3′,2′:3,4]pyrrolo[1,2- a ]quinoxalines and pyrido[2′,3′:5,6]pyrazino[2,1- a ]isoindoles, were synthesized through an aza-substitution on the already active isoindolo-quinoxaline system and in particular in the position 7 or 4 of the isoindole moiety and in position 5 of the quinoxaline portion. All new compounds were screened by the National Cancer Institute (Bethesda, MD) against a panel of 60 human tumor cell lines. Biological results of the most active derivatives, with pGI 50 values between 7.09 and 7.27, confirmed the importance of the presence of methoxy substituents for biological activity. The ant…

QuinoxalineIsoindolesAzaisoindolo-quinoxalinesStereochemistryAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Antineoplastic Agents; Apoptosis; Aza Compounds; Cell Line Tumor; Cell Proliferation; Dose-Response Relationship Drug; Drug Screening Assays Antitumor; Humans; Isoindoles; Molecular Structure; Quinoxalines; Structure-Activity Relationship; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; Pharmacology; Medicine (all)ApoptosisAntineoplastic AgentsAntiproliferative activityIsoindolesRing (chemistry)Drug Screening AssaysCell LineDose-Response Relationshipchemistry.chemical_compoundStructure-Activity RelationshipQuinoxalineCell Line TumorQuinoxalinesDrug DiscoverymedicineMoietyHumansAntiproliferative activity; Apoptosis; Azaisoindolo-quinoxalines; DNA interaction; Isoindolo-azaquinoxalines; Quinoxalines; Drug Discovery3003 Pharmaceutical Science; Organic Chemistry; PharmacologyCell ProliferationPharmacologyAza CompoundsAzaisoindolo-quinoxalineTumorDose-Response Relationship DrugMolecular StructureDrug Discovery3003 Pharmaceutical ScienceMedicine (all)Organic ChemistryApoptosiBiological activityGeneral MedicineAntitumorCell cycleSettore CHIM/08 - Chimica FarmaceuticaDNA interactionSettore ING-IND/22 - Scienza E Tecnologia Dei MaterialiMechanism of actionchemistryIsoindolo-azaquinoxalineDrug Screening Assays Antitumormedicine.symptomDrugIsoindoleIsoindolo-azaquinoxalines
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The influence of substitution in the quinoxaline nucleus on 1,3-dipolar cycloaddition reactions

2013

The reaction mechanism of 1,3-dipolar cycloadditions of both symmetric and unsymmetric benzo-condensed diazines with a nitrilimine dipole, to give two different mono- and bis-cycloadducts, in tetrahydrofuran (THF) solution, was studied by DFT calculatio ns. The results obtained show that each 1,3-dipolar cycloaddition reaction always proceeds by a two steps mechanism, in which the first intermediate shows only one covalent bond between the beta carbon of the nitrilimine and the aromatic nitrogen of the diazine molecule. The structure and energy content of the two transition states of the two cycloaddition steps, in the case of the unsymmetric benzo-condensed diazine, nicely explains why the…

Settore CHIM/03 - Chimica Generale E InorganicaSettore CHIM/08 - Chimica FarmaceuticaDFT calculations 13-Dipolar cycloaddition reactions Quinoxalines Reaction mechanism
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SYNTHESIS OF TETRACYCLIC SYSTEMS WITH POTENT ANTITUMOR ACTIVITY

2011

TETRACYCLIC SYSTEMS QUINOXALINES ANTITUMOR ACTIVITYQUINOXALINESTETRACYCLIC SYSTEMS; QUINOXALINES; ANTITUMOR ACTIVITYTETRACYCLIC SYSTEMSSettore CHIM/08 - Chimica FarmaceuticaANTITUMOR ACTIVITY
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