5-(5-BROMOTHIEN-2-YL)-2'-DEOXYURIDINE AND 5-(5-CHLOROTHIEN-2-YL)-2'-DEOXYURIDINE ARE EQUIPOTENT TO (E)-5-(2-BROMOVINYL)-2'-DEOXYURIDINE IN THE INHIBITION OF HERPES-SIMPLEX VIRUS TYPE-I REPLICATION

被引:87
|
作者
WIGERINCK, P [1 ]
PANNECOUQUE, C [1 ]
SNOECK, R [1 ]
CLAES, P [1 ]
DECLERCQ, E [1 ]
HERDEWIJN, P [1 ]
机构
[1] CATHOLIC UNIV LEUVEN,REGA INST MED RES,MINDERBROEDERSSTR 10,B-3000 LOUVAIN,BELGIUM
关键词
D O I
10.1021/jm00112a011
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
2'-Deoxyuridines with a five-membered heterocyclic substituent in the 5-position were synthesized by palladium-catalyzed coupling reactions of 5-iodo-2'-deoxyuridine with the activated heteroaromatics. Further modification of the compound with the 5-thien-2-yl substituent gave 5-(5-bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothienyl-2-yl)-2'-deoxyuridine. Both compounds show potent and selective activity against herpes simplex virus type 1 and varicella-zoster virus.
引用
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页码:2383 / 2389
页数:7
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