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1-[ω-(苯氧基)烷基]尿嘧啶衍生物及其类似物的合成及抗 HCMV 活性。

Synthesis and anti-HCMV activity of 1-[ω-(phenoxy)alkyl]uracil derivatives and analogues thereof.

机构信息

Department of Pharmaceutical & Toxicological Chemistry, Volgograd State Medical University, Pavshikh Bortsov Sq., 1, Volgograd 400131, Russia.

出版信息

Bioorg Med Chem. 2013 Jul 15;21(14):4151-7. doi: 10.1016/j.bmc.2013.05.009. Epub 2013 May 16.

Abstract

HCMV infection represents a life-threatening condition for immunocompromised patients and newborn infants and novel anti-HCMV agents are clearly needed. In this regard, a series of 1-[ω-(phenoxy)alkyl]uracil derivatives were synthesized and examined for antiviral properties. Compounds 17, 20, 24 and 28 were found to exhibit highly specific and promising inhibitory activity against HCMV replication in HEL cell cultures with EC50 values within 5.5-12μM range. Further studies should be undertaken to elucidate the mechanism of action of these compounds and the structure-activity relationship for the linker region.

摘要

HCMV 感染对免疫功能低下的患者和新生儿来说是一种危及生命的情况,显然需要新型的抗 HCMV 药物。在这方面,我们合成了一系列 1-[ω-(苯氧基)烷基]尿嘧啶衍生物,并对其抗病毒特性进行了研究。在 HEL 细胞培养物中,化合物 17、20、24 和 28 对 HCMV 复制表现出高度特异和有前景的抑制活性,EC50 值在 5.5-12μM 范围内。应进一步进行研究,以阐明这些化合物的作用机制以及连接子区域的构效关系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd8b/7127185/60c5917fa3e2/fx1.jpg

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