Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors

Jie Zhang; Wenfang Xu; Ailin Liu; Guanhua Du

doi:10.2174/157340608784325151

Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors

Jie Zhang
, Wenfang Xu
, Ailin Liu
, Guanhua Du

Shandong University
Chinese Academy of Medical Sciences

科研成果: 期刊稿件 › 文章 › 同行评审

9 引用（Scopus）

摘要

A series of pyrrolidine derivatives were designed and synthesized in good yields starting from commercially available 4-hydroxy-L-proline using a suitable synthetic strategy. And their ability to inhibit neuraminidase was evaluated. These compounds showed potent inhibitory activity against influenza A (H3N2) neuraminidase. Within this series, four compounds, 6e, 9c, 9f and 10e, have the good potency (IC₅₀=1.56-2.4μM) which is compared to the NA inhibitor oseltamivir (IC₅₀=1.06μM), and could be used as lead compound in the future.

源语言	英语
页（从-至）	206-209
页数	4
期刊	Medicinal Chemistry
卷	4
期	3
DOI	https://doi.org/10.2174/157340608784325151
出版状态	已出版 - 5月 2008
已对外发布	是

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title = "Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors",

abstract = "A series of pyrrolidine derivatives were designed and synthesized in good yields starting from commercially available 4-hydroxy-L-proline using a suitable synthetic strategy. And their ability to inhibit neuraminidase was evaluated. These compounds showed potent inhibitory activity against influenza A (H3N2) neuraminidase. Within this series, four compounds, 6e, 9c, 9f and 10e, have the good potency (IC50=1.56-2.4μM) which is compared to the NA inhibitor oseltamivir (IC50=1.06μM), and could be used as lead compound in the future.",

keywords = "Influenza virus, Inhibitor, Neuraminidase, Pyrrolidine derivatives",

author = "Jie Zhang and Wenfang Xu and Ailin Liu and Guanhua Du",

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T1 - Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors

AU - Zhang, Jie

AU - Xu, Wenfang

AU - Liu, Ailin

AU - Du, Guanhua

PY - 2008/5

Y1 - 2008/5

N2 - A series of pyrrolidine derivatives were designed and synthesized in good yields starting from commercially available 4-hydroxy-L-proline using a suitable synthetic strategy. And their ability to inhibit neuraminidase was evaluated. These compounds showed potent inhibitory activity against influenza A (H3N2) neuraminidase. Within this series, four compounds, 6e, 9c, 9f and 10e, have the good potency (IC50=1.56-2.4μM) which is compared to the NA inhibitor oseltamivir (IC50=1.06μM), and could be used as lead compound in the future.

AB - A series of pyrrolidine derivatives were designed and synthesized in good yields starting from commercially available 4-hydroxy-L-proline using a suitable synthetic strategy. And their ability to inhibit neuraminidase was evaluated. These compounds showed potent inhibitory activity against influenza A (H3N2) neuraminidase. Within this series, four compounds, 6e, 9c, 9f and 10e, have the good potency (IC50=1.56-2.4μM) which is compared to the NA inhibitor oseltamivir (IC50=1.06μM), and could be used as lead compound in the future.

KW - Influenza virus

KW - Inhibitor

KW - Neuraminidase

KW - Pyrrolidine derivatives

UR - https://www.scopus.com/pages/publications/45149122533

U2 - 10.2174/157340608784325151

DO - 10.2174/157340608784325151

M3 - 文章

C2 - 18473912

AN - SCOPUS:45149122533

SN - 1573-4064

VL - 4

SP - 206

EP - 209

JO - Medicinal Chemistry

JF - Medicinal Chemistry

IS - 3

ER -

Design, synthesis, and preliminary evaluation of new pyrrolidine derivatives as neuraminidase inhibitors

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