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:	Stereochemistry medicine.drug_class Peptidomimetic Clinical Biochemistry Plasmepsin Protozoan Proteins Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Phenylbutyrate Antimalarials Structure-Activity Relationship Drug Discovery medicine Structure–activity relationship Aspartic Acid Endopeptidases Computer Simulation Protease Inhibitors Molecular Biology chemistry.chemical_classification Binding Sites biology Chemistry fungi Organic Chemistry Aromatic amine Ethylenediamines Phenylbutyrates Thiazoles Enzyme inhibitor biology.protein Molecular Medicine
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::be82fad5ed0038bbb55473008e6d5a93 https://pubmed.ncbi.nlm.nih.gov/20634066 Zobrazit plný text záznamu Full Text from ScienceDirect