Probing The P3' Pocket Of Stromelysin With Piperazic Acid Analogs

Da Nugiel, K Jacobs,Cp Decicco,Dj Nelson,Ra Copeland, Kd Hardman

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1995）

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摘要

The preparation and SAR of several piperazic acid-based stromelysin (MMP-3) inhibitors is presented. The standard P3' methyl amide substituent can be replaced by other carboxy based substituents and maintain good binding affinity. Removal of a hydrogen-bond acceptor results in a 30-fold decrease in activity.

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关键词

binding affinity,hydrogen bond

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