The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. On this 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.
Romeo, R., Iannazzo, D., Veltri, L., Gabriele, B., Macchi, B., Frezza, C., et al. (2019). Pyrimidine 2,4-Diones in the design of new HIV RT inhibitors. MOLECULES, 24(9), 1718-1731 [10.3390/molecules24091718].
Pyrimidine 2,4-Diones in the design of new HIV RT inhibitors
Veltri L.;Macchi B.;Frezza C.;
2019-05-02
Abstract
The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. On this 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.| File | Dimensione | Formato | |
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