0000000000206532

AUTHOR

Erik De Clercq

0000-0002-2985-8890

showing 5 related works from this author

Synthesis and pharmacological evaluation of several ring-contracted amantadine analogs

2008

Graphical abstract Several bisnoradamantylamines and noradamantylamines have been synthesized and their antiviral, trypanocidal, NMDA receptor antagonist, and dopamine reuptake inhibitory activities have been studied.

RimantadineStereochemistryDopamineeducationClinical BiochemistryPharmaceutical Sciencemacromolecular substancesPharmacologymedicine.disease_causeAntiviral AgentsReceptors N-Methyl-D-AspartateBiochemistryChemical synthesisArticleInhibitory Concentration 50DogsPolycyclic compoundMemantineTrypanosomiasisDopamineDrug DiscoveryAmantadinemedicineInfluenza A virusAnimalsNMDA receptor antagonistMolecular BiologyCells Culturedchemistry.chemical_classificationChemistryOrganic ChemistryAmantadinePolycyclic cage compoundsBiological activityInfluenzanervous systemInfluenza A virusMolecular MedicineNMDA receptormedicine.drugBioorganic & Medicinal Chemistry
researchProduct

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
researchProduct

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)
researchProduct

Synthesis and antiproliferative activity of 2'-O-allyl-1-beta-D-arabynofuranosyl-uracil, -cytosine and -adenine

1997

Abstract With the aim to design potential inhibitors of ribonucleotide reductase (RR), 2′-O-allyl-β-D-arabinofuranosyl-uracil ( 4 ), -cytosine ( 7 ) and -adenosine ( 10 ) were prepared and evaluated for their cytostatic activity against Molt4/C8, CEM and L1210 cell lines. Although our preliminary data do not allow to assess if RR is the intracellular target, the results point to differences in the (anti)metabolic behavior of these compounds. This study also offers a general synthesis of 2′-O-allyl-β-D-arabinofuranosyl nucleosides for potential applications in the preparation of 2′-O-allyl-β-D-oligoarabino nucleotides.

chemistry.chemical_classificationStereochemistryorganic chemicalsOrganic ChemistryClinical Biochemistryfood and beveragesPharmaceutical ScienceUracilBiological activityBiochemistryAdenosineChemical synthesischemistry.chemical_compoundRibonucleotide reductasechemistryBiochemistryDrug DiscoverymedicineMolecular MedicineNucleotideMolecular BiologyNucleosideCytosinemedicine.drug
researchProduct

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
researchProduct