Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold L-arginine as amino-peptidase N/CD13 inhibitors

A series of bi- or tri-peptide analogues with the scaffold L-arginine were designed, synthesized and evaluated for their inhibitory activities against amino-peptidase N (APN) and metalloproteinase-2 (MMP-2). The primary activity assay showed that all the compounds exhibited higher inhibitory activities against APN than MMP-2. Within this series, compounds C6 and C7 (IC50 = 4.2 and 4.3 mu M) showed comparable APN inhibitory activities with the positive control bestatin (IC50 = 3.8 mu M). (C) 2009 Elsevier Ltd. All rights reserved.