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

Authors :: Sergey N. Kochetkov
Alexander V. Ivanov
Denis A. Babkov
Maria P. Paramonova
Mikhail S. Novikov
Jan Balzarini
Christophe Pannecouque
Alexander Ozerov
Vladimir T. Valuev-Elliston
Source :: Pharmaceutical Chemistry Journal. 47:459-463
Publication Year :: 2013
Publisher :: Springer Science and Business Media LLC, 2013.
Abstract: 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.

Subjects :: Pharmacology
Anti hiv 1
chemistry.chemical_classification
Alkane
Pyrimidine
Stereochemistry
Alkene
Pharmacology toxicology
Uracil
Reverse transcriptase
chemistry.chemical_compound
chemistry
Drug Discovery
Alkyl

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