Design, synthesis, and preliminary activity evaluation of novel peptidomimetics as aminopeptidase N/CD13 inhibitors

X Li, J Wang, L Zhang, W Xu

Index: Li, Xun; Wang, Junli; Zhang, Lei; Xu, Wenfang Archiv der Pharmazie, 2011 , vol. 344, # 8 p. 494 - 504

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Citation Number: 5

Abstract

Abstract The synthesis of a series of novel N-α-galloylated isoglutamic acid γ-amide peptidomimetics is described. Their enzymatic inhibition against aminopeptidase N (APN/CD13) and matrix metalloproteinase-2 (MMP-2) was tested. The preliminary activity assay revealed that most of the compounds displayed selective inhibition against APN as compared with MMP-2, with IC 50 values in a micromolar range. Within this series, ...