Potent carboxylate inhibitors of stromelysin containing P2' piperazic acids and P1' biaryl moeities

被引：13

作者：

Cherney, RJ

Decicco, CP

Nelson, DJ

Wang, L

Meyer, DT

Hardman, KD

Copeland, RA

Arner, EC

机构：

[1] DuPont Merck Pharmaceutical Co., Experimental Station, Wilmington

[2] Chem. Phys. Sci. Inflammatory D., Experimental Station, Wilmington

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(97)00308-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several carboxylate derivatives with variation at the P1' residue were synthesized and evaluated as stromelysin (MMP-3) inhibitors. Compounds containing a biphenyl moiety at P1' were found to be potent inhibitors of MMP-3. An X-ray crystal structure of the most potent compound, carboxylate 19, revealed an important interaction between the inhibitor's biphenyl and histidine 224 in the S1' pocket of MMP-3. (C) 1997 Elsevier Science Ltd.

引用

页码：1757 / 1762

页数：6

共 18 条

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