Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5′-thioadenosine derivatives.: Antiviral effects

被引:7
作者
Guillerm, G
Guillerm, D
Vandenplas-Vitkowski, C
Glapski, C
De Clercq, E
机构
[1] UFR Sci, Chim Bioorgan Lab, UMR 6519, F-51687 Reims 2, France
[2] Katholieke Univ Leuven, Rega Inst Med Res, Louvain, Belgium
关键词
D O I
10.1016/S0960-894X(03)00279-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Synthesis of 5'-S-vinyl-5'-thioadenosine 5, 5'-S-ethynyl-5'-thioadenosine 7 and 5'-S-cyano-5'-thioadenosine 9 is described. Incubation of AdoHcy hydrolase with 5, 7 and 9 resulted in time- and concentration-dependent inactivation of the enzyme and partial depletion of its NAD(+) content. From these results and characterisation of metabolites released during the inactivation process, hypothetical mechanisms are suggested. The antiviral activity of 5, 7 and 9 was examined. Significant activities were noted with 5 against Vaccinia, Junin and Taccaribe viruses. (C) 2003 Elsevier Science Ltd. All rights reserved.
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页码:1649 / 1652
页数:4
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