| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Fiscal Year 2012: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Outline of Final Research Achievements |
We planed structure-based drug design of new diketo acid derivatives targeting the subunit PAN of RNA polymerase of influenza virus and inhibiting the metalloenzyme by chelation. The phenyl and biphenyl diketo acids with a nitro or carboxy group as hydrogen bond acceptor were synthesized. Of these, a biphenyl diketo acid with a carboxy group showed the most potent inhibitory effect against the nuclease activity of PAN. A good correlation between the inhibitory activity of the diketo acids with a carboxy group and their docking energies was shown. In addition, single crystals of PAN were obtained, and the X-ray crystallographic analysis was successfully done.
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