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

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• 作者：Cherney ; Robert J. ; Decicco ; Carl P. ; Nelson ; David J. ; Li ; Wang ; Meyer ; Dayton T. ; Hardman ; Karl D. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1997
• 出版时间：July 8, 1997
• 年：1997
• 卷：7
• 期：13
• 页码：1757-1762
• 全文大小：265 K

文摘

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.