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

被引：27

作者：

Novikov, Mikhail S. ^{[1
]}

Babkov, Denis A. ^{[1
]}

Paramonova, Maria P. ^{[1
]}

Khandazhinskaya, Anastasia L. ^{[2
]}

Ozerov, Alexander A. ^{[1
]}

Chizhov, Alexander O. ^{[3
]}

Andrei, Graciela ^{[4
]}

Snoeck, Robert ^{[4
]}

Balzarini, Jan ^{[4
]}

Seley-Radtke, Katherine L. ^{[5
]}

机构：

[1] Volgograd State Med Univ, Dept Pharmaceut & Toxicol Chem, Volgograd 400131, Russia

[2] Russian Acad Sci, VA Engelhardt Mol Biol Inst, Moscow 119991, Russia

[3] Russian Acad Sci, Zelinsky Inst Organ Chem, Moscow 119991, Russia

[4] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium

[5] Univ Maryland Baltimore Cty, Dept Chem & Biochem, Baltimore, MD 21250 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2013年 / 21卷 / 14期

基金：

俄罗斯基础研究基金会;

关键词：

HCMV; Uracil derivatives; Antiviral; Nonnucleoside; Nucleobase; HUMAN CYTOMEGALOVIRUS HCMV; ZOSTER-VIRUS VZV; ANTIVIRAL ACTIVITY; PHARMACOKINETIC PROPERTIES; BIOLOGICAL-ACTIVITY; INHIBITORS; POTENT; GANCICLOVIR; RETINITIS; INFECTION;

D O I：

10.1016/j.bmc.2013.05.009

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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-[omega-(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 5.5-12 mu M range. Further studies should be undertaken to elucidate the mechanism of action of these compounds and the structure-activity relationship for the linker region. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：4151 / 4157

页数：7

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