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Bioorg Med Chem Lett. 2010 Apr 15;20(8):2497-9. doi: 10.1016/j.bmcl.2010.02.111. Epub 2010 Mar 4.

Identification of very potent inhibitor of human aminopeptidase N (CD13).

Author information

1
Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wroclaw University of Technology, Wybrzeze Wyspianskiego, Wroclaw, Poland.

Abstract

In this Letter we describe broad comparision studies toward rat, pig, and human aminopeptidase N (CD13) orthologs using phosphinate inhibitors related in structure to hydroxamic acids. This SAR approach yielded a very potent inhibitor of human aminopeptidase N: alpha(1)-amino-3-phenylpropyl(alpha(2)-hydroxy-3-phenylpropyl)phosphinic acid with an IC(50)=60 nM.

PMID:
20307982
DOI:
10.1016/j.bmcl.2010.02.111
[Indexed for MEDLINE]

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