Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA

被引：63
|
作者：
Ballatore, C
McGuigan, C
De Clercq, E
Balzarini, J
机构：
[1] Univ Wales Coll Cardiff, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales
[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 08期
关键词：
D O I：
10.1016/S0960-894X(01)00128-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Some novel amidate prodrugs of PMEA and PMPA have been synthesised and tested in vitro for their biological activity. Compound 5 in particular showed greatly enhanced antiviral potency compared with the parent nucleotide analogue. In vitro enzymatic studies and structure-activity relationships indicate that the degradation mechanism of such prodrugs may be the same as that described for the phosphoramidate triesters of nucleotide analogues. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1053 / 1056
页数：4
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