Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors.

Research paper by Qiang Q Wang, Maoying M Chen, Huawei H Zhu, Jie J Zhang, Hao H Fang, Binghe B Wang, Wenfang W Xu

Indexed on: 10 May '08Published on: 10 May '08Published in: Bioorganic & Medicinal Chemistry


A series of novel l-lysine derivatives were designed, synthesized, and assayed for their inhibitory activities on amino-peptidase N (APN)/CD13 and matrix metalloproteinase-2 (MMP-2). The preliminary biological test showed that most of the compounds displayed a high inhibitory activity against MMP-2 and a low activity against APN except compound B6 which exhibited good potency (IC(50)=13.2microM) similar with APN inhibitor Bestatin (IC(50)=15.5microM), and could be used as lead compound in the future.