| Project/Area Number |
21790121
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
HIDAKA Koushi Kyoto Pharmaceutical University, 薬学部, 助教 (30445960)
|
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| Project Period (FY) |
2009 – 2010
|
| Project Status |
Completed (Fiscal Year 2010)
|
| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2010: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2009: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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| Keywords | 感染症 / 酵素 / 阻害剤 / 分子設計 / 分子認識 / アスパラギン酸プロテアーゼ / HIVプロテアーゼ / プラスメプシン / 架橋水 |
|---|
| Research Abstract |
Pseudo-symmetric protease inhibitors which have unique "HMC-hyrazide" as a transition state mimic to set multiple bridging waters were designed. Although the synthetic pseudo-symmetric compounds exhibited some reduction of inhibitory activity against multi-mutated HIV protease, the activity reduction of derivatives with oxamide at both terminals were relatively less. The pseudo-symmetric compounds also exhibited HTLV-I protease inhibitory activity.
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