新型赖氨酸衍生物作为氨基肽酶N/CD13抑制剂的设计、合成及定量构效关系研究
Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors.
作者信息
Wang Qiang, Chen Maoying, Zhu Huawei, Zhang Jie, Fang Hao, Wang Binghe, Xu Wenfang
机构信息
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong 250012, PR China.
出版信息
Bioorg Med Chem. 2008 May 15;16(10):5473-81. doi: 10.1016/j.bmc.2008.04.012. Epub 2008 Apr 11.
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.
设计、合成了一系列新型L-赖氨酸衍生物，并检测了它们对氨肽酶N（APN）/CD13和基质金属蛋白酶-2（MMP-2）的抑制活性。初步生物学试验表明，除化合物B6外，大多数化合物对MMP-2表现出高抑制活性，对APN表现出低活性。化合物B6表现出与APN抑制剂Bestatin（IC50 = 15.5μM）相似的良好活性（IC50 = 13.2μM），未来可用作先导化合物。
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