Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase

被引：39

作者：

Jeng, AY ^{[1
]}

Chou, M ^{[1
]}

Parker, DT ^{[1
]}

机构：

[1] Novartis Pharmaceut, Metab & Cardiovasc Dis Res, Summit, NJ 07901 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 08期

关键词：

D O I：

10.1016/S0960-894X(98)00142-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structural requirements of sulfonamide-based hydroxamic acid 1 for inhibition of macrophage metalloelastase (MME) were investigated. A short aliphatic group at the R-2 position together with an aromatic group at the R-3 position significantly improved the inhibitory activity. Compounds 32, 34, and 40 were the most potent inhibitors of MME with IC50 values between 5 and 6 nM. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：897 / 902

页数：6

共 15 条

[11]

ROQUES BP, 1993, PHARMACOL REV, V45, P87

[12] ELASTIN DEGRADATION BY HUMAN ALVEOLAR MACROPHAGES - A PROMINENT ROLE OF METALLOPROTEINASE ACTIVITY [J].

SENIOR, RM ;

CONNOLLY, NL ;

CURY, JD ;

WELGUS, HG ;

CAMPBELL, EJ .

AMERICAN REVIEW OF RESPIRATORY DISEASE, 1989, 139 (05) :1251-1256

[13]

SHAPIRO SD, 1992, J BIOL CHEM, V267, P4664

[14]

SHAPIRO SD, 1993, J BIOL CHEM, V268, P23824

[15] EMPHYSEMA - THE 1ST 2 CENTURIES - AND BEYOND - A HISTORICAL OVERVIEW, WITH SUGGESTIONS FOR FUTURE-RESEARCH .2. [J].

SNIDER, GL .

AMERICAN REVIEW OF RESPIRATORY DISEASE, 1992, 146 (06) :1615-1622

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