Synthesis of New Cyclic and Acyclic 5-Halouridine Derivatives as Potential Antiviral Agents

被引：8
|
作者：
Elshehry, Mohamed F. [1 ,2 ]
Balzarini, Jan [3 ]
Meier, Chris [1 ]
机构：
[1] Univ Hamburg, Fac Sci, Dept Chem, D-20146 Hamburg, Germany
[2] Natl Res Ctr, Pesticide Dept, Cairo 12622, Egypt
[3] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
SYNTHESIS-STUTTGART | 2009年 / 05期
关键词：
bioorganic chemistry; drugs; antiviral agents; nucleosides; glycosylation; IMMUNODEFICIENCY-VIRUS TYPE-1; GENERAL SYNTHESIS; N-GLYCOSIDES; HIV; NUCLEOSIDES; TOXICITY; SERIES; AZT;
D O I：
10.1055/s-0028-1083369
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
The synthesis of new cyclic and acyclic nucleoside analogues was achieved by alkylation of 5-halogenated 6-(2,4-dichlorophenoxymethyl)pyrimidine-2,4-dione following the Vorbruggen coupling procedure. Nucleoside analogues of the 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT)-type were obtained as well as analogues of ganciclovir, acyclovir, and ribonucleosides. All compounds were tested against a variety of viruses. Three of the new compounds were potent and selective anti-HIV-1 inhibitors.
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页码：841 / 847
页数：7
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