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

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