Author/Authors :
David A. Nugiel، نويسنده , , Kim Jacobs، نويسنده , , Carl P. Decicco، نويسنده , , David J. Nelson، نويسنده , , Robert A. Copeland، نويسنده , , Karl D. Hardman، نويسنده ,
Abstract :
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.