Synthesis and anti-influenza evaluation of polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en derivatives

被引：56
作者：
Honda, T
Yoshida, S
Arai, M
Masuda, T
Yamashita, M
机构：
[1] Sankyo Co Ltd, Med Chem Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
[2] Sankyo Co Ltd, Biol Res Labs, Shinagawa Ku, Tokyo 1408710, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 15期
关键词：
D O I：
10.1016/S0960-894X(02)00330-X
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We synthesized polyvalent sialidase inhibitors bearing 4-guanidino-Neu5Ac2en analogues on the polyglutamic acid back bone, via a spacer of alkyl ether at the C-7 position. These multivalent conjugates 9 and 10 showed enhancement of antiviral activity against infuenza A virus and more potent efficacy in vivo relative to a monomeric sialidase inhibitor. (C) 2002 Elsevier Science Ltd. All rights reserved.
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页码：1929 / 1932
页数：4
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