1331960-95-2Relevant articles and documents
Design, synthesis, and preliminary activity evaluation of novel peptidomimetics as aminopeptidase N/CD13 inhibitors
Li, Xun,Wang, Junli,Zhang, Lei,Xu, Wenfang
experimental part, p. 494 - 504 (2011/11/04)
The synthesis of a series of novel N-α-galloylated isoglutamic acid I-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 IC50 values in a micromolar range. Within this series, compound 4 (IC 50a=10.2a±a.9μM) demonstrated comparable APN inhibition as compared with the positive control bestatin (IC 50a=a13.1aa0.7aμM), which might be a promising lead for further molecular optimizations. A new series of bi-peptide analogues containing amino acid or organic acid residues as elongated hydrophobic substituents inserting into S1 or S1 pocket was designed. Most of the target compounds showed potent and selective activities against APN/CD13 as compared with MMP-2. Compound 4 was comparable to bestatin and could be used as a potential lead for further development of APNIs.