Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase
Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase
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DOI：
10.1016/s0960-894x(98)00142-5
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发表时间：
1998-04-21
影响因子：
2.7
通讯作者：
Parker, DT
中科院分区：
文献类型：
--
作者：
Jeng, AY;Chou, M;Parker, DT
研究了磺胺基异羟肟酸1对巨噬细胞金属弹性蛋白酶(MME)抑制作用的结构要求。R-2位上的短链脂肪基和R-3位上的芳香基团显著提高了抑制活性。化合物32、34和40对MME的抑制作用最强，IC50值在5~6 nM之间。(C)1998爱思唯尔科学有限公司。保留所有权利。
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.