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Synthesis and in-vitro activity of 4'-modified analogues of ddA as potent anti-HIV agents.

机译:ddA的4'-修饰类似物作为有效的抗HIV药物的合成及体外活性。

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摘要

This paper reports the synthesis of novel 4'-hydrophobic pocket deoxythreosyl C-nucleosides. The key threose-like intermediates 9 and 14 were constructed from acyclic ketone derivatives, respectively. The antiviral activities of the synthesized compounds against the HIV-1, HSV-1, HSV-2, and HCMV viruses were evaluated. The 9-deaza-adenine derivatives 10 and 20 showed good anti-HIV activity without exhibiting significant cytotoxicity.
机译:本文报道了新型4'-疏水口袋脱氧苏糖基C-核苷的合成。关键的苏糖状中间体9和14分别由无环酮衍生物构成。评估了合成化合物对HIV-1,HSV-1,HSV-2和HCMV病毒的抗病毒活性。 9-脱氮-腺嘌呤衍生物10和20显示出良好的抗HIV活性,而没有表现出明显的细胞毒性。

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