Novel inhibitors of influenza sialidase related to GG167 - Synthesis of 4-amino and guanidino-4H-pyran-2-carboxylic acid-6-propylamides; Selective inhibitors of influenza A virus sialidase

被引：58

作者：

Sollis, SL

Smith, PW

Howes, PD

Cherry, PC

Bethell, RC

机构：

[1] GLAXO WELLCOME RES & DEV LTD,MED RES CTR,ENZYME MED CHEM 2,STEVENAGE SG1 2NY,HERTS,ENGLAND

[2] GLAXO WELLCOME RES & DEV LTD,MED RES CTR,ENZYME PHARMACOL,STEVENAGE SG1 2NY,HERTS,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 15期

关键词：

D O I：

10.1016/0960-894X(96)00318-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

N-Propylcarboxamides 1a,b-3a,b have been synthesised from 2,3-didehydro-2,4-dideoxy-4-amino-N-acetylneuraminic acid 4. The tertiary amides 2a,b-3a,b are highly potent but selective inhibitors of influenza A sialidase. The exceptional inhibitory activity of the dipropylamides 3a and 3b against influenza A shows that the 6-dipropylcarboxamide substituent is preferable to the polar glycerol sidechain found in the related sialidase inhibitors GG167 and 4. Copyright (C) 1996 Elsevier Science Ltd

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页码：1805 / 1808

页数：4

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