Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution |
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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 |
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| Affiliation: | 1. Department of Medicinal Chemistry, Center for Frontier Research in Medicinal Science, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8412, Japan;2. Department of Biology and Johns Hopkins Malaria Research Institute, Johns Hopkins University, Baltimore, MD 21218, USA |
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| 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. |
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