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.

引用

页码：841 / 847

页数：7

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