ANTI-HIV AND ANTI-HBV ACTIVITIES OF L-2',3'-DIDEOXYNUCLEOSIDE ANALOGS - DDC, 5FDDC, 5-AZA DDC AND DDG

被引:0
|
作者
MANSOUR, TS
TSE, A
CHARRON, M
机构
[1] GLAXO WELLCOME PLC,DEPT VIROL,STEVENAGE SG1 2NY,HERTS,ENGLAND
[2] BIOCHEM THERAPEUT INC,LAVAL,PQ H7V 4A7,CANADA
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Dideoxynucleoside analogues are amongst the most important inhibitors of reverse transcriptase (RT), a key enzyme encoded by HIV and involved in its replication.(1) Compelling evidence has supported the notion that some analogues with the L-absolute configuration in the heterosubstituted nucleoside analogues are potent antiviral agents. (-)-2'-Deoxy-3'-thiacytidine(2) (3TC((TM)), lamivudine), its 5-fluoro analogue(3) (-)-FTC and (-)-dioxolane C ((-)-BCH-204)(4) are prototypes with beta-L-configuration possessing potent anti-HIV and anti-HBV activities. In particular, substantial selectivity is demonstrated with 3TC((M)), which is currently in advanced clinical trials for the treatment of AIDS and hepatitis-B infections.(5)
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页码:417 / 425
页数:9
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