Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold L-arginine as amino-peptidase N/CD13 inhibitors
Source: Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript, Available online 22 November 2009
Jiajia, Mou , Hao, Fang , Yingzi, Liu , Luqing, Shang , Qiang, Wang , ...
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, compound C6 and C7 (IC50= 4.2 and 4.3 μM) showed comparable APN inhibitory activities with the positive control bestatin (IC50= 3.8μM).
