Synthesis and biological activity of new 6-benzylisocytosine derivatives: non-nucleoside HIV-1 reverse transcriptase inhibitors

Synthesis and biological activity of new 6-benzylisocytosine derivatives: non-nucleoside HIV-1 reverse transcriptase inhibitors

New 6-benzylisocytosine derivatives were synthesized by aminolysis of 6-benzyl-2-(methylsulfanyl)pyrimidin-4(3 H )-ones with aliphatic aromatic and cage-structured amines. Some of the synthesized compounds appeared to be effective HIV-1 reverse transcriptase inhibitors. Among these, 6-(2,6-difluorob...

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Veröffentlicht in:Pharmaceutical chemistry journal 2012-10, Vol.46 (7), p.397-401
Hauptverfasser: Valuev-Elliston, V. T., Ivanov, A. V., Orlinson, B. S., Gerasimov, E. N., Brunilina, L. L., Kochetkov, S. N., Novakov, I. A., Navrotskii, M. B.
Format: Artikel
Sprache:eng
Schlagworte:
Anti-HIV agents
Antiviral agents
DNA polymerases
HIV (Viruses)
Medicine
Nucleosides
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
Reverse transcriptase inhibitors
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Zusammenfassung:New 6-benzylisocytosine derivatives were synthesized by aminolysis of 6-benzyl-2-(methylsulfanyl)pyrimidin-4(3 H )-ones with aliphatic aromatic and cage-structured amines. Some of the synthesized compounds appeared to be effective HIV-1 reverse transcriptase inhibitors. Among these, 6-(2,6-difluorobenzyl)-5-methyl-2-[(2-phenylethyl)amino]pyrimidin-4(3 H )-one showed the most pronounced inhibitory properties, being nine times more effective than the reference anti-HIV drug nevirapine.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-012-0808-y