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Literature DB >> 18467109

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

Qiang Wang¹, Maoying Chen, Huawei Zhu, Jie Zhang, Hao Fang, Binghe Wang, Wenfang Xu.

Abstract

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.

Entities: Chemical Gene

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Year: 2008 PMID： 18467109 DOI： 10.1016/j.bmc.2008.04.012

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

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Cited

3 in total

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

1. Activity screening and structure-activity relationship of the hit compounds targeting APN/CD13.

2. Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.

3. Design, synthesis and primary activity evaluation of L-arginine derivatives as amino-peptidase N/CD13 inhibitors.