Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44, Wenhuaxi Road, Ji'nan, Shandong 250012, PR China.
Bioorg Med Chem. 2010 Jan 15;18(2):887-95. doi: 10.1016/j.bmc.2009.11.036. Epub 2009 Nov 22.
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).
设计、合成了一系列具有 l-精氨酸骨架的双肽或三肽类似物，并评价了它们对氨基肽酶 N（APN）和基质金属蛋白酶-2（MMP-2）的抑制活性。初步活性测定表明，所有化合物对 APN 的抑制活性均高于 MMP-2。在该系列中，化合物 C6 和 C7（IC50=4.2 和 4.3μM）对 APN 的抑制活性与阳性对照物金精三羧酸（bestatin，IC50=3.8μM）相当。
