| Budget Amount *help |
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2013: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
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| 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.
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