Search results for "NRTI"

showing 10 items of 14 documents

Abacavir induces platelet-endothelium interactions by interfering with purinergic signalling: A step from inflammation to thrombosis.

2017

The controversy connecting Abacavir (ABC) with cardiovascular disease has been fuelled by the lack of a credible mechanism of action. ABC shares structural similarities with endogenous purines, signalling molecules capable of triggering prothrombotic/proinflammatory programmes. Platelets are leading actors in the process of thrombosis. Our study addresses the effects of ABC on interactions between platelets and other vascular cells, while exploring the adhesion molecules implicated and the potential interference with the purinergic signalling pathway. The effects of ABC on platelet aggregation and platelet-endothelium interactions were evaluated, respectively, with an aggregometer and a flo…

0301 basic medicineBlood PlateletsEndotheliumPlatelet AggregationAnti-HIV AgentsInflammationPharmacologyBiologyProinflammatory cytokine03 medical and health sciences0302 clinical medicinePlatelet Adhesivenessplatelet-endothelium interactionsVirologymedicineHumansPlatelet030212 general & internal medicinePlatelet activationPharmacologyInflammationCell adhesion moleculePurinergic receptorDeoxyguanine NucleotidesThrombosisPurinergic signallingIntercellular Adhesion Molecule-1Platelet ActivationAbacavirNRTIsDideoxynucleosidesCell biologycardiovascular diseasesP-Selectin030104 developmental biologymedicine.anatomical_structureCardiovascular DiseasesPurinesEndothelium Vascularmedicine.symptomSignal TransductionAntiviral research
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Efficacy and tolerability of switching to a dual therapy with darunavir/ritonavir plus raltegravir in HIV-infected patients with HIV-1 RNA ≤50 cp/…

2017

Background: Nucleos(t)ide reverse transcriptase inhibitors (NRTI) toxicity may represent a threat for long-term success of combined antiretroviral therapy. Some studies have suggested a possible improvement of NRTI-related toxicity after switching to NRTI-sparing regimens. Objectives: We aimed to explore the efficacy and tolerability of switching to darunavir/ritonavir (DRV/r) plus raltegravir (RAL) while having a viral load (VL) ≤50 copies/mL in the clinical setting. Study design: Treatment-experienced HIV 1-infected patients enrolled in the ICONA Foundation Study cohort were included if they switched their current regimen to DRV/r + RAL with a HIV-RNA ≤50 copies/mL. Different defin…

0301 basic medicineMaleHIV InfectionsAntiretroviral therapy; Darunavir/ritonavir; Efficacy; NRTI-sparing regimen; Raltegravir; Tolerability; Microbiology (medical); Infectious DiseasesAntiretroviral therapy; Darunavir/ritonavir; Efficacy; NRTI-sparing regimen; Raltegravir; Tolerability; Adult; Anti-HIV Agents; Cohort Studies; Darunavir; Drug Therapy Combination; Female; HIV Infections; HIV-1; Humans; Italy; Male; Middle Aged; RNA Viral; Raltegravir Potassium; Ritonavir; Viral LoadGastroenterologyCohort StudiesAntiretroviral therapy; Darunavir/ritonavir; Efficacy; NRTI-sparing regimen; Raltegravir; Tolerability0302 clinical medicineMedicineNRTI-sparing regimen030212 general & internal medicineViralDarunavireducation.field_of_studyLamivudineGeneral MedicineMiddle AgedViral LoadTolerabilityAntiretroviral therapyInfectious DiseasesTolerabilityItalyCombinationRNA ViralDrug Therapy CombinationFemaleViral loadmedicine.drugAdultMicrobiology (medical)medicine.medical_specialtyEfficacyAnti-HIV Agents030106 microbiologyPopulationDarunavir/ritonavir; Raltegravir; Efficacy; Tolerability; Antiretroviral therapy; NRTI-sparing regimenSettore MED/17 - MALATTIE INFETTIVELower riskNO03 medical and health sciencesDrug TherapyInternal medicineRaltegravir PotassiumHumanseducationDarunavirRitonavirbusiness.industryDarunavir/ritonavirRaltegravirRaltegravirHIV-1RNARitonavirbusinessAntiretroviral therapy; Darunavir/ritonavir; Efficacy; NRTI-sparing regimen; Raltegravir; Tolerability;
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Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.

2002

Several 2,3-diaryl-1,3-thiazolidine-4-thione derivatives and 2,3-diaryl-1,3-thiazolidin-4-ones bearing a methyl group at C-5 position have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

23-Diaryl-13-thiazolidine-4-thioneAnti-HIV activity23-Diaryl-13-thiazolidin-4-oneStereochemistryAnti-HIV AgentsCell SurvivalPharmaceutical ScienceVirus ReplicationChemical synthesischemistry.chemical_compoundInhibitory Concentration 50Structure-Activity RelationshipThiadiazolesDrug DiscoveryThiadiazolesmedicineTumor Cells CulturedStructure–activity relationshipHumansAnti hiv activityReverse-transcriptase inhibitorGeneral MedicineSettore CHIM/08 - Chimica FarmaceuticaIn vitrochemistryNNRTIsLactamHIV-1EpimerMethyl groupmedicine.drugFarmaco (Societa chimica italiana : 1989)
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Long-term CD4+ T-cell count evolution after switching from regimens including HIV nucleoside reverse transcriptase inhibitors (NRTI) plus protease in…

2011

Abstract Background Data regarding CD4+ recovery after switching from protease inhibitor (PI)-based regimens to regimens not containing PI are scarce. Methods Subjects with virological success on first-PI-regimens who switched to NNRTI therapy (NNRTI group) or to nucleoside reverse transcriptase (NRTI)-only (NRTI group) were studied. The effect of the switch on the ongoing CD4+ trend was assessed by two-phase linear regression (TPLR), allowing us to evaluate whether a change in the CD4+ trend (hinge) occurred and the time of its occurrence. Furthermore, we described the evolution of the frequencies in CD4-count classes across four relevant time-points (baseline, before and immediately after…

AdultCD4-Positive T-LymphocytesMalemedicine.medical_treatmentProtease InhibitorHuman immunodeficiency virus (HIV)CD4+ T-cellHIV InfectionsBiologymedicine.disease_causeSettore MED/17 - MALATTIE INFETTIVENucleoside Reverse Transcriptase InhibitorTimelcsh:Infectious and parasitic diseasesZidovudineRetrospective Studieimmune system diseasesAntiretroviral Therapy Highly ActivemedicineHumansProtease inhibitor (pharmacology)HIV InfectionProtease Inhibitorslcsh:RC109-216Retrospective StudiesHIV; CD4+ T-cellProteaseCd4 t cellDrug SubstitutionBackground dataHIVvirus diseasesMiddle AgedVirologyHIV; AIDS; CD4; NRTIReverse Transcriptase InhibitorCD4 Lymphocyte CountInfectious DiseasesCD4-Positive T-LymphocyteReverse Transcriptase InhibitorsRitonavirFemaleAdult; Antiretroviral Therapy Highly Active; CD4 Lymphocyte Count; CD4-Positive T-Lymphocytes; Female; HIV Infections; Humans; Male; Middle Aged; Protease Inhibitors; Retrospective Studies; Reverse Transcriptase Inhibitors; Time; Drug Substitution; Infectious Diseasesmedicine.drugHumanResearch Article
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Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones

2002

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Anti hiv activityAnti-HIV activityAnti-HIV Agents23-Diaryl-13-thiazolidin-4-oneChemistryStereochemistryHuman immunodeficiency virus (HIV)Pharmaceutical ScienceGeneral MedicineVirus ReplicationRing (chemistry)medicine.disease_causeChemical synthesisIn vitroCell LineThiazoleschemistry.chemical_compoundHIV-2Drug DiscoveryHIV-1NNRTIsLactammedicineHumansIl Farmaco
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Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and teste…

2003

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a variously substituted phenyl ring at N-3 have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Anti-HIV activity23-Diaryl-13-thiazolidin-4-oneNNRTIs
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Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Anti-HIV activity23-diaryl-13-thiazolidin-4-oneAnti-HIV AgentsCell SurvivalT-LymphocytesDrug Evaluation PreclinicalPharmaceutical SciencePharmacologyVirus ReplicationStructure-Activity RelationshipDrug DiscoveryStructure–activity relationshipHumansCytotoxicityCell survivalAnti hiv activityMolecular StructureAnti hivChemistryvirus diseasesSettore CHIM/08 - Chimica FarmaceuticaReverse transcriptaseIn vitroThiazolesViral replicationHIV-2HIV-1NNRTIsReverse Transcriptase Inhibitors
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Involvement of nitric oxide in the mitochondrial action of efavirenz: a differential effect on neurons and glial cells

2014

Abstract The anti-human immunodeficiency virus (HIV) drug efavirenz (EFV) alters mitochondrial function in cultured neurons and glial cells. Nitric oxide (NO) is a mediator of mitochondrial dysfunction associated with HIV central nervous system symptoms. We show that EFV promotes inducible nitric oxide synthase (iNOS) expression in cultured glial cells and generated NO undermines their mitochondrial function, as inhibition of NOS partially reverses this effect. EFV inhibits mitochondrial Complex I in both neurons and glia; however, when the latter cells are treated for longer periods, other mitochondrial complexes are also affected in accordance with the increased NO production. These findi…

CyclopropanesNNRTIEfavirenzAnti-HIV AgentsCentral nervous systemNitric Oxide Synthase Type IIMitochondrionBiologyNitric OxideNitric oxideCell Linechemistry.chemical_compoundMediatornitric oxidemedicineImmunology and AllergyHumansNeuronsNeurotoxicityelectron transport chainHIVefavirenzmedicine.diseasecentral nervous systemCell biologyBenzoxazinesMitochondriaNitric oxide synthasemitochondriaInfectious Diseasesmedicine.anatomical_structurechemistryAlkynesImmunologybiology.proteinNeurogliaNeuroglia
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De novo drug design and synthesis of new HIV-1 NNRTIs

2002

HIV-1 NNRTIs
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Design and synthesis of new HIV-1 NNRTIs

2003

HIV-1 NNRTIs
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