Synthesis and Anti-HIV-1 Activity of 1-[ω-(Phenoxy)Alkyl and -Alkenyl]Uracil Derivatives

Synthesis and Anti-HIV-1 Activity of 1-[ω-(Phenoxy)Alkyl and -Alkenyl]Uracil Derivatives

1-[ω-(Phenoxy)alkyl and -alkenyl]uracil derivatives were synthesized via condensation of equimolar amounts of 2,4- bis (trimethylsilyloxy)pyrimidine and 1-halo-ω-(phenoxy)alkane or -alkene in order to discover new non-nucleoside inhibitors of HIV-1 reverse transcriptase. Their anti-HIV-1 activity wa...

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Veröffentlicht in:Pharmaceutical chemistry journal 2013-12, Vol.47 (9), p.459-463
Hauptverfasser: Paramonova, M. P., Babkov, D. A., Valuev-Elliston, V. T., Ivanov, A. V., Kochetkov, S. N., Pannecouque, C., Ozerov, A. A., Balzarini, J., Novikov, M. S.
Format: Artikel
Sprache:eng
Schlagworte:
Antiviral agents
DNA polymerases
Highly active antiretroviral therapy
HIV (Viruses)
Human immunodeficiency virus 1
Medicine
Olefins
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Pyrimidines
Search for New Drugs
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Zusammenfassung:1-[ω-(Phenoxy)alkyl and -alkenyl]uracil derivatives were synthesized via condensation of equimolar amounts of 2,4- bis (trimethylsilyloxy)pyrimidine and 1-halo-ω-(phenoxy)alkane or -alkene in order to discover new non-nucleoside inhibitors of HIV-1 reverse transcriptase. Their anti-HIV-1 activity was studied in CEM-cell culture and against HIV-1 reverse transcriptase. It was found that several compounds exhibited marked activity.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-013-0980-8