Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution

Bioorganic & Medicinal Chemistry Letters
Takuya MiuraYoshiaki Kiso

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.

References

Jan 7, 1972·Nature·C A HomewoodV C Baggaley
Aug 4, 2009·Bulletin of the World Health Organization·Anthony BurtonMaureen Birmingham

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Citations

Mar 6, 2012·BMC Genomics·Timothy G LilburnYufeng Wang
May 28, 2013·International Journal of Cell Biology·Jasmin LindnerCarsten Wrenger
Apr 2, 2015·European Journal of Medicinal Chemistry·Nirnoy Dan, Soumendranath Bhakat
May 5, 2011·Biochimica Et Biophysica Acta·Prasenjit BhaumikAlexander Wlodawer
Dec 3, 2014·Molecular and Biochemical Parasitology·Huogen XiaoRickey Y Yada
Dec 2, 2015·Acta Crystallographica. Section F, Structural Biology Communications·Rosario RecachaKaspars Tars

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