6533b86efe1ef96bd12cc80e

RESEARCH PRODUCT

Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

A CarboneJan BalzariniAlba ChimirriA. RaoErik De ClercqChristophe PannecouquePietro MonforteMaria ZappalàAnna Maria Monforte

subject

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

description

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).

http://hdl.handle.net/10447/12191