The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. Onthis basis, a series of pyrimidine-2,4-diones linked to an isoxazolidine nucleus have been synthesized and tested as nucleoside analogs, endowed with potential anti-HIV (human immunodeficiency virus) activity. Compounds 6a-c, characterized by the presence of an ethereal group at C-3, show HIV reverse transcriptase (RT) inhibitor activity in the nanomolar range as well as HIV-infection inhibitor activity in the low micromolar with no toxicity. In the same context, compound 7b shows only a negligible inhibition of RT HIV.

Pyrimidine 2,4-Diones in the design of new HIV RT inhibitors

Veltri L.;Gabriele B.;Macchi B.;
2019-01-01

Abstract

The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. Onthis basis, a series of pyrimidine-2,4-diones linked to an isoxazolidine nucleus have been synthesized and tested as nucleoside analogs, endowed with potential anti-HIV (human immunodeficiency virus) activity. Compounds 6a-c, characterized by the presence of an ethereal group at C-3, show HIV reverse transcriptase (RT) inhibitor activity in the nanomolar range as well as HIV-infection inhibitor activity in the low micromolar with no toxicity. In the same context, compound 7b shows only a negligible inhibition of RT HIV.
2019
Biological activity; HIV RT inhibitors; Molecular docking; Pyrimidine-2,4-dione derivatives; Reverse nucleosides; Chemistry Techniques, Synthetic; HIV-1; Humans; Models, Molecular; Molecular Structure; Protein Binding; Pyrimidines; Quantitative Structure-Activity Relationship; Reverse Transcriptase Inhibitors; Drug Design
File in questo prodotto:
Non ci sono file associati a questo prodotto.

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.11770/298539
 Attenzione

Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo

Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus 31
  • ???jsp.display-item.citation.isi??? 28
social impact