Non-peptidic inhibitors of human neutrophil elastase: The design and synthesis of sulfonanilide-containing inhibitors

被引：32

作者：

Imaki, K ^{[1
]}

Okada, T ^{[1
]}

Nakayama, Y ^{[1
]}

Nagao, Y ^{[1
]}

Kobayashi, K ^{[1
]}

Sakai, Y ^{[1
]}

Mohri, T ^{[1
]}

Amino, T ^{[1
]}

Nakai, H ^{[1
]}

Kawamura, M ^{[1
]}

机构：

[1] ONO PHARMACEUT CO LTD, DEPT MED CHEM, MINASE RES INST, MISHIMA, OSAKA 618, JAPAN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1996年 / 4卷 / 12期

关键词：

D O I：

10.1016/S0968-0896(96)00216-7

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements for metabolic stabilization are also discussed. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2115 / 2134

页数：20

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