Synthesis and anti-influenza evaluation of orally active bicyclic ether derivatives related to zanamivir

被引：57

作者：

Masuda, T

Shibuya, S

Arai, M

Yoshida, S

Tomozawa, T

Ohno, A

Yamashita, A

Honda, T

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 | 2003年 / 13卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(02)01039-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We synthesized bicyclic ether sialidase inhibitors Such as tetrahydro-furan-2-yl. tetrahydro-pyran-2-yL and oxepan-2-yl derivatives related to zanamivir. These compounds substituted by diol at the C-3' and C-4' positions resulted in the retention of low nanomolar inhibitory activities against not only influenza A virus sialidase but also influenza A virus in cell culture. Compound I la in particular showed comparable efficacy in vivo relative to that of oseltamivir phosphate. (C) 2003 Elsevier Science Ltd. All rights reserved.

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页码：669 / 673

页数：5

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