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Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors.

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.

SUBMITTER: Romeo R

PROVIDER: S-EPMC6539630 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors.

Romeo Roberto R Iannazzo Daniela D Veltri Lucia L Gabriele Bartolo B Macchi Beatrice B Frezza Caterina C Marino-Merlo Francesca F Giofrè Salvatore V SV

Molecules (Basel, Switzerland) 20190502 9

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 <b>6a</b>-<b>c</b>, 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 inhibit ...[more]

PMID: 31052607

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