The world's scientific and social network for malaria professionals
Subscribe to free Newsletter | 11110 malaria professionals are enjoying the free benefits of MalariaWorld today

2-aminoethylamino

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

July 28, 2010 - 07:56 -- Kabogo Ndegwa
Author(s): 
Takuya Miura, Koushi Hidaka, Tsuyoshi Uemura, Keisuke Kashimoto, Yuto Hori, Yuko Kawasaki, Adam J. Ruben, Ernesto Freire, Tooru Kimura, Yoshiaki Kiso
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 20, Issue 16, 15 August 2010, Pages 4836-4839

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 (Ki <0.1 nM).

Medical Condition: 
Medical Treatment: 
Subscribe to RSS - 2-aminoethylamino