| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371365 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
We attached 2-aminoethylamino groups to allophenylnorstatine-containing plasmepsin (Plm) inhibitors and investigated SAR of the methyl or ethyl substitutions on the amino groups. Unexpectedly, compounds 22 (KNI-10743) and 25 (KNI-10742) exhibited extremely potent Plm II inhibitory activities (Ki <0.1 nM). Moreover, among our peptidomimetic Plm inhibitors, we identified the compounds with the highest antimalarial activity using a SYBR Green I-based fluorescence assay.
Graphical abstractAttachments of 2-aminoethylamino substituents to an allophenylnorstatine-containing plasmepsin inhibitor enhanced both plasmepsin inhibitory and antimalarial activities.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso,