Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.

Basic Information

ID: ALA1144647

Journal: Bioorg Med Chem Lett

Title: Additional interaction of allophenylnorstatine-containing tripeptidomimetics with malarial aspartic protease plasmepsin II.

Authors: Hidaka K, Kimura T, Tsuchiya Y, Kamiya M, Ruben AJ, Freire E, Hayashi Y, Kiso Y.

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 K(i) values of less than 0.1n M suggesting successful hydrophobic interactions.

CiteXplore: 17400453

DOI: 10.1016/j.bmcl.2007.03.052

Patent ID: