title: Design, synthesis, and preliminary activity evaluation of novel peptidomimetics as aminopeptidase N/CD13 inhibitors.
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, compound 4 (IC(50) = 10.2 ± 0.9 µM) demonstrated comparable APN inhibition as compared with the positive control bestatin (IC(50) = 13.1 ± 0.7 µM), which might be a promising lead for further molecular optimizations.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Ji'nan, Shandong Province, P.R. China.
authors.forename: Xun
authors.initials: X
authors.lastname: Li
authors.forename: Junli
authors.initials: J
authors.lastname: Wang
authors.forename: Lei
authors.initials: L
authors.lastname: Zhang
authors.forename: Wenfang
authors.initials: W
authors.lastname: Xu
mesh_terms: D018826:CD13 Antigens / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015195:Drug Design; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D057786:Peptidomimetics / Q000032:analysis / Q000138:chemical synthesis* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D057786:Peptidomimetics; D018826:CD13 Antigens