一类新的核苷酸类似物作为抗hcmv药物的设计和SAR研究。

N Nguyen-Ba, L Chan, M Quimpère, N Turcotte, N Lee, H Mitchell, J Bédard
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引用次数: 7

摘要

我们已经开发了一类新的2-膦酸1,3-二恶唑烷核苷酸类似物,其鸟嘌呤衍生物显示出弱的抗hcmv活性。进一步的SAR研究表明,与更昔洛韦和hmpc相比,四氢呋喃类似物的顺式和反式鸟嘌呤衍生物在体外和体内都是有效的抗hcmv药物。
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Design and SAR study of a novel class of nucleotide analogues as potent anti-HCMV agents.

We have developed a novel class of 2-phosphonate 1,3-dioxolane nucleotide analogues, from which the guanine derivative displayed weak anti-HCMV activity. Further SAR studies led to the identification of both cis and trans guanine derivatives of tetrahydrofuran analogues as potent anti-HCMV agents, both in vitro and in vivo, compared to ganciclovir and HPMPC.

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