Synthesis and influenza virus sialidase inhibitory activity of analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) modified in the glycerol side-chain

被引：38

作者：

Andrews, DM ^{[1
]}

Cherry, PC ^{[1
]}

Humber, DC ^{[1
]}

Jones, PS ^{[1
]}

Keeling, SP ^{[1
]}

Martin, PF ^{[1
]}

Shaw, CD ^{[1
]}

Swanson, S ^{[1
]}

机构：

[1] Glaxo Wellcome Med Res Ctr, Dept Med Chem, Stevenage SG1 2NY, Herts, England

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 1999年 / 34卷 / 7-8期

关键词：

influenza virus sialidase neuraminidase Zanamivir; antiviral activity;

D O I：

10.1016/S0223-5234(00)80026-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Analogues of 4-Guanidino-Neu5Ac2en (Zanamivir) have been prepared containing carbamate substituents at the 7-hydroxy position. (4S,SR,6R)-5-Acetylamino-6-{1R-[(6-aminohexyl)carbamoyloxyl-2R,3-dihydroxypropyl}-4-guanidino-5,6-dihydro-4H-pyran-2-carboxylic acid and (4S,SR,6R)-5-Acetylamino-6-{1R-Cheptylcarbamoyloxyl-2R,3-dihydroxypropyl}-4-guanidino-5,6-dihydro4H-pyran-2-carboxylic acid were the two analogues possessing activity comparable to Zanamivir, showing potent inhibition of influenza virus sialidases and good antiviral activity in vitro. (C) 1999 Editions scientifiques ct medicales Elsevier SAS.

引用

页码：563 / 574

页数：12

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