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

Research paper by Jiajia J Mou, Hao H Fang, Yingzi Y Liu, Luqing L Shang, Qiang Q Wang, Lei L Zhang, Wenfang W Xu

Indexed on: 09 Dec '09Published on: 09 Dec '09Published in: Bioorganic & Medicinal Chemistry



Abstract

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 (IC(50)=4.2 and 4.3microM) showed comparable APN inhibitory activities with the positive control bestatin (IC(50)=3.8microM).