Search results for "Anti hiv"

showing 9 items of 9 documents

Anti-HIV Agents Derived from the ent-Kaurane Diterpenoid Linearol

2002

Twenty-six semisynthetic ent-kaurane derivatives of linearol (1) have been investigated for their anti-HIV effects. Five compounds (4, 7, 11, 25, and 26) showed significant activity against HIV replication in H9 lymphocyte cells with EC(50) values in the range <0.1-3.11 microg/mL. With TI values of 163 and 184, compounds 4 and 25 are especially promising for further development as potential anti-HIV agents.

Magnetic Resonance SpectroscopyAnti-HIV AgentsStereochemistryLymphocyteEnt kaurane diterpenoidHuman immunodeficiency virus (HIV)Pharmaceutical ScienceBiologymedicine.disease_causeAnalytical Chemistrychemistry.chemical_compoundDrug DiscoverymedicineCombinatorial Chemistry TechniquesHumansLymphocytesPharmacologyMolecular StructureAnti hivOrganic ChemistryHIVbiology.organism_classificationIn vitroTerpenoidmedicine.anatomical_structureComplementary and alternative medicinechemistryLentivirusSideritisMolecular MedicineDiterpenesDiterpeneJournal of Natural Products
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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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A QSAR study investigating the potential anti-HIV-1 effect of some acyclovir and ganciclovir analogs

2009

A QSAR study, involving the use of calculated physical-chemical properties (TSAR TM ), and the use of a neural network approach (TSAR TM ), has been performed on the potential anti-HIV-1 activity of a series of Acyclovir and Ganciclovir analogs. Model obtained allows reliable predictions for the anti-HIV-1 activity of these derivatives, and showed that the presence of the Ganciclovir chain in triazolopyrrolopyrimidine and pyrimidopyrrolopyrimidine series seems to increase the antiviral effect.

GanciclovirAnti hiv 1Quantitative structure–activity relationshipStereochemistryChemistryOrganic ChemistrymedicineQSAR neural network BMLR anti-HIV-1 activityvirus diseasesPharmacologySettore CHIM/08 - Chimica Farmaceuticamedicine.drug
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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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A review of natural and modified betulinic, ursolic and echinocystic acid derivatives as potential antitumor and anti-HIV agents.

2003

The aim of this review is to update current knowledge on the betulinic, ursolic and echinocystic acids and their natural and semisynthetic analogs, focussing on their cytotoxic and anti-HIV activities. Then, the last results of the authors' team on unusual semisynthetic derivatives of these triterpenoids will be presented in order to establish structure/activity relationships.

PharmacologyMolecular StructureAnti hivChemistryAnti-HIV AgentsTumor cellsAntineoplastic AgentsGeneral MedicinePharmacologyTriterpenesStructure-Activity RelationshipTriterpenoidDrug DiscoveryHIV-1Tumor Cells CulturedStructure–activity relationshipHumansEchinocystic acidOleanolic AcidBetulinic AcidPentacyclic TriterpenesHT29 CellsMini reviews in medicinal chemistry
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QSAR Modeling ANTI-HIV-1 Activities by Optimization of Correlation Weights of Local Graph Invariants

2004

Results of using descriptors calculated with the correlation weights (CWs) of local graph invariants for modeling of anti-HIV-1 potencies of two groups of reverse transcriptase (RT) inhibitors are reported. Presence of different chemical elements in molecular structure of the inhibitors and the presence of Morgan extended connectivity values of zeroth-, first- and second order have been examined as local graph invariants in the labeled hydrogen-filled graphs. By Monte Carlo method optimization procedure, values of the CWs which produce as large values as possible of correlation coefficient between the numerical data on the anti-HIV-1 potencies and values of the descriptors on the training s…

Anti hiv 1Quantitative structure–activity relationshipCorrelation coefficientGeneral Chemical EngineeringMonte Carlo methodGeneral ChemistryCondensed Matter PhysicsGraphCombinatoricsCorrelationZeroth law of thermodynamicsModeling and SimulationOrder (group theory)General Materials ScienceInformation SystemsMathematicsMolecular Simulation
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Anti-HCV, anti-GOR, and autoimmunity

1992

biologybusiness.industryAnti hivImmunopathologyImmunologybiology.proteinMedicineGeneral MedicineAntibodybusinessmedicine.disease_causeVirologyAutoimmunityThe Lancet
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Demonstration of antibodies to the surface (anti-p41) and core proteins (anti-p24) of the human immunodeficiency virus (HIV) in individuals positive …

1987

Diagnosis of infection with the human immunodeficiency virus (HIV) relies on the demonstration of antibody to this virus. Occasionally, the combined analysis of sera using ELISA and western blot reveals false-positive results. We have compared a newly developed test to detect antibodies to the core (anti-p24) and surface (anti-p41) proteins of HIV with the established tests described above. Anti-p24 and anti-p41 were negative in three individuals positive for anti-HIV by ELISA and immunoblot; they had a low risk to acquire HIV infection and were clinically and immunologically normal and suspected false positive previously. In 62 individuals at risk, anti-p41 was always positive while anti-p…

MaleRiskRetroviridae Proteins OncogenicHuman immunodeficiency virus (HIV)Retroviridae ProteinsEnzyme-Linked Immunosorbent AssayHIV Antibodiesmedicine.disease_causeAntibodies ViralVirusAcquired immunodeficiency syndrome (AIDS)Western blotViral Envelope ProteinsAntibody SpecificityDrug DiscoverymedicineHumansGenetics (clinical)Acquired Immunodeficiency Syndromebiologymedicine.diagnostic_testAnti hivvirus diseasesHIVCore proteinGeneral Medicinemedicine.diseaseVirologyHIV Envelope Protein gp41Immunologybiology.proteinMolecular MedicineFemaleAntibodyKlinische Wochenschrift
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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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