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

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2013-07, Vol.21 (14), p.4151-4157
Main Authors: Novikov, Mikhail S., Babkov, Denis A., Paramonova, Maria P., Khandazhinskaya, Anastasia L., Ozerov, Alexander A., Chizhov, Alexander O., Andrei, Graciela, Snoeck, Robert, Balzarini, Jan, Seley-Radtke, Katherine L.
Format: Article
Language:English
Subjects:
Antiviral
Antiviral activity
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
antiviral properties
cell culture
Cells, Cultured
Cytomegalovirus - drug effects
HCMV
Human cytomegalovirus
Humans
mechanism of action
neonates
Nonnucleoside
Nucleobase
patients
Receptors, Virus - drug effects
Structure-Activity Relationship
structure-activity relationships
Uracil - chemical synthesis
Uracil - chemistry
Uracil - pharmacology
Uracil derivatives
Virus Replication - drug effects
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Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2013.05.009