Dipartimento di Scienze chimiche, biologiche, farmaceutiche ed ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, Italy.
Dipartimento di Ingegneria, Università di Messina, Contrada Di Dio, 98166 Messina, Italy.
Molecules. 2019 May 2;24(9):1718. doi: 10.3390/molecules24091718.
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 -, 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 shows only a negligible inhibition of RT HIV.
嘧啶核是开发抗逆转录病毒药物的多功能核心。在此基础上，合成了一系列连接异噁唑烷核的嘧啶-2,4-二酮，并将其作为核苷类似物进行了测试，具有潜在的抗 HIV（人类免疫缺陷病毒）活性。化合物 - ，其特征在于在 C-3 处具有醚基团，在纳摩尔范围内表现出 HIV 逆转录酶 (RT) 抑制剂活性，并且在低微摩尔范围内具有 HIV 感染抑制剂活性，而没有毒性。在相同的背景下，化合物 仅对 HIV RT 表现出可忽略的抑制作用。
