Novel phenylpiperazine derivatives as dual cytokine regulators with TNF-α suppressing and IL-10 augmenting activity

被引：7

作者：

Hanano, T

Adachi, K

Aoki, Y

Morimoto, H

Naka, Y

Hisadome, M

Fukuda, T

Sumichika, H

机构：

[1] Yoshitomi Pharmaceut Ind Ltd, Div Pharmaceut Res, Drug Discovery Labs, Iruma, Saitama 3580026, Japan

[2] Yoshitomi Pharmaceut Ind Ltd, Div Pharmaceut Res, Drug Dev Labs, Yoshitomi, Fukuoka 8718550, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 09期

关键词：

D O I：

10.1016/S0960-894X(00)00128-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Phenylpiperazine derivatives were synthesized as dual cytokine regulators with TNF-alpha suppressing and IL-10 augmenting activity. Lead optimization led to compound 5k having the potent regulatory activity and demonstrating remarkable protective effects against the lethal challenge of LPS in mice, suggesting that 5k would be a promising drug candidate for the treatment of TNF-alpha associated diseases including septic shock. (C) 2000 Elsevier Science Ltd. All rights reserved.

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页码：875 / 879

页数：5

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