Use of a pharmacophore model to discover a new class of influenza endonuclease inhibitors

被引：144

作者：

Parkes, KEB

Ermert, P

Fässler, J

Ives, J

Martin, JA

Merrett, JH

Obrecht, D

Williams, G

Klumpp, K

机构：

[1] Roche Discovery Welwyn, Welwyn Garden City AL7 3AY, Herts, England

[2] Polyphor Ltd, CH-4123 Allschwil, Switzerland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 07期

关键词：

D O I：

10.1021/jm020334u

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Data from both our own and literature studies of the biochemistry and inhibition of influenza virus endonuclease was combined with data on the mechanism of action and the likely active site mechanism to propose a pharmacophore. The pharmacophore was used to design a novel structural class of inhibitors, some of which were found to have activities similar to that of known influenza endonuclease inhibitors and were also antiviral in cell culture.

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收藏

页码：1153 / 1164

页数：12

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