| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1366546 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Based on a highly potent allophenylnorstatine-containing inhibitor, KNI-10006, against the plasmepsins of Plasmodium falciparum, we synthesized a series of tripeptide-type compounds with various N-terminal moieties and evaluated their inhibitory activities against plasmepsin II. Certain phenylacetyl derivatives exhibited extremely high affinity with Ki values of less than 0.1 nM suggesting successful hydrophobic interactions.
Graphical abstractA series of allophenylnorstatine-containing tripeptidic compounds were synthesized with various N-terminal phenylacetyl moieties. Certain derivatives exhibited extremely potent inhibitory activity against plasmepsin II.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Koushi Hidaka, Tooru Kimura, Yumi Tsuchiya, Mami Kamiya, Adam J. Ruben, Ernesto Freire, Yoshio Hayashi, Yoshiaki Kiso,