Development of antimalarial agents through a design of reversely binding protease inhibitors

2015 Fiscal Year Final Research Report

• Project/Area Number: 25460163
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Kobe Gakuin University
• Principal Investigator: Hidaka Koushi 神戸学院大学, 薬学部, 講師 (30445960)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: マラリア / HIV / 治療薬 / プロテアーゼ阻害剤 / 分子設計 / プラスメプシン

Outline of Final Research Achievements

To develop new antimalarial agents, plasmepsin inhibitors possessing an unnatural amino acid, allophenylnorstatine, which bind with in opposite way to that of substrate, were synthesized. The known inhibitors with basic auxiliary moiety were tested against chloroquine-resistant P. falciparum to exhibit large activity attenuation. Therefore, the new basic moieties, except 2-aminoethylamino group which is structurally similar to chloroquine, were incorporated. The synthesized compounds were found to be potent against the drug resistant parasite.

Free Research Field

医薬品化学