2-(2,6-dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as nonnucleoside HIV-1 reverse trascriptase inhibitors

Anna Carbone, De Clercq, Zappalà, Pannecouque, Jan Balzarini, Monforte, Anna Carbone, Chimirri, Monforte, Rao

Risultato della ricerca: Articlepeer review

110 Citazioni (Scopus)

Abstract

Several 1,3-thiazolidin-4-ones bearing a 2,6-dihalophenyl group at C-2 and a substituted pyrimidin-2-yl ring at the N-3 were synthesised and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of human immunodeficiency virus type-1 (HIV-1) replication at 10–40 nM concentrations with minimal cytotoxicity. Structure–activity relationship studies revealed that the nature of the substituents at the 2 and 3 positions of the thiazolidinone nucleus had a significant impact on the in vitro anti-HIV activity of this class of potent antiretroviral agents. The compounds had significantly reduced activity against the characteristic NNRTI-resistant virus mutants (bearing the K103N and Y181C RT mutations), thereby acting as non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors (NNRTIs).
Lingua originaleEnglish
pagine (da-a)79-84
Numero di pagine6
RivistaAntiviral Research
Volume63
Stato di pubblicazionePublished - 2004

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Virology

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