|Budget Amount *help
¥55,000,000 (Direct Cost: ¥55,000,000)
Fiscal Year 2005: ¥15,000,000 (Direct Cost: ¥15,000,000)
Fiscal Year 2004: ¥15,000,000 (Direct Cost: ¥15,000,000)
Fiscal Year 2003: ¥15,000,000 (Direct Cost: ¥15,000,000)
Fiscal Year 2002: ¥10,000,000 (Direct Cost: ¥10,000,000)
Current situation of the malaria becomes serious more and more and recently, drug-resistant Plasmodium falciparum malaria parasites, human infected severe malaria, has increased drug-resistant P. falciparum malaria.
Our research objective is development of new antiamalarial drug against drug-resistant P. falciparum and our study is advanced for the purpose of contributing to the malaria control. For the dissolve the antimalarial action, we used new antimalarial organic compounds, endoperoxides, with molecular biology and computor based drug-target techniques. Our final goal of research is control of malaria from the on earth.
The research result of this study is shown at the following.
We synthesized the 150 g of 1,2,4,5-tetraoxacycloalkane (N-89) including improvement of synthtic steps for supply of cheap price in the malaria endemic areas and research of suitable solvent for good manufactured practice during synthetic steps.
It's antimalarial test for monkey malaria parasite infected monkey was done. As a result, N-89 has high antimalarial activities for monkey malaria with no any cytotoxic effect. Finally, malarial parasites infected monkey cured for N-89 treatment of oral route. Also our compound has no side effect treatment with 2,000 mg/kg of N-89, weight loss, biological composition of blood, behavior, against rat.
Pharmacokinetic study of N-89, blood concentration level of N-89 was 1×10^<-7> M, and this concentration was also kept 5 hours after N-89 treatment. Blood level of N-89 concentration was sufficient for kill the malaria parasite in the blood. During pharmacokinetic parameter analysis, our compound have short half time in the blood stream (t_<1/2>=45 min) and shows the high bioavailability (BA=58.6%). In conclusion, Our compoud can be expected as a new antimalarial drug.