These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.
    Author: Miura T, Hidaka K, Uemura T, Kashimoto K, Hori Y, Kawasaki Y, Ruben AJ, Freire E, Kimura T, Kiso Y.
    Journal: Bioorg Med Chem Lett; 2010 Aug 15; 20(16):4836-9. PubMed ID: 20634066.
    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 (K(i)<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.
    [Abstract] [Full Text] [Related] [New Search]