Novel 5,5-disubstitutedpyrimidine-2,4,6-trione as selective MMP inhibitors

被引:40
作者
Foley, LH [1 ]
Palermo, R [1 ]
Dunten, P [1 ]
Wang, P [1 ]
机构
[1] Hoffmann La Roche Inc, Roche Res Ctr, Nutley, NJ 07110 USA
关键词
D O I
10.1016/S0960-894X(01)00104-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The 5.5-disubstitutedpyrimidine-2,4.6-trione represent a new class of MIL IP inhibitors showing selectivity for the gelatinases A and B, collagenase-3, and human neutrophil collagenase. The SAR presented here is in good agreement with an X-ray structure of compound 5 bound to the catalytic domain of stromelysin-1. While of the barbiturate structural class, compound 5 did not show any toxic or sedative effects. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:969 / 972
页数:4
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