Lactate cannot substitute for alanine in D4T-based anti-HIV nucleotide prodrugs - Despite efficient esterase-mediated hydrolysis.

被引：9
作者：
McGuigan, C
Cahard, D
Ballatore, C
Siddiqui, A
De Clercq, E
Balzarini, J
机构：
[1] Cardiff Univ, Welsh Sch Pharm, Cardiff CF1 3XF, S Glam, Wales
[2] Katholieke Univ Leuven, Rega Inst Med Res, B-3000 Louvain, Belgium
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 21期
关键词：
D O I：
10.1016/S0960-894X(98)00530-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
As part of our on-going effort to deliver masked phosphates of antiviral nucleosides inside living cells we have previously discovered that amino acid-derived phosphoramidates are particularly effective. Here we report that lactate analogues, with a simple change of bridging nitrogen for oxygen, are virtually inactive as antiviral agents and apparently do not achieve intracellular nucleoside phosphate delivery. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.
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收藏
页码：2949 / 2954
页数：6
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