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

Autor: Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yoshiaki Kiso, Takuya Miura, Tooru Kimura, Koushi Hidaka
Rok vydání: 2010
Předmět:
Zdroj: Bioorganicmedicinal chemistry letters. 20(16)
ISSN: 1464-3405
Popis: 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)
Databáze: OpenAIRE
Popis
Abstrakt: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)
ISSN:14643405