| Project/Area Number |
10102010
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| Research Category |
Grant-in-Aid for Specially Promoted Research
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| Allocation Type | Single-year Grants |
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| Review Section |
Chemistry
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| Research Institution | Waseda University |
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Principal Investigator |
TATSUTA Kuniaki Waseda University, School of Science and Engineering, Professor, 理工学部, 教授 (40051627)
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| Co-Investigator(Kenkyū-buntansha) |
NAKADA Masahisa Waseda University, School of Science and Engineering, Professor, 理工学部, 教授 (50198131)
SHIMIZU Isao Waseda University, School of Science and Engineering, Professor, 理工学部, 教授 (50134820)
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| Project Period (FY) |
1998 – 2001
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| Project Status |
Completed (Fiscal Year 2001)
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| Budget Amount *help |
¥283,800,000 (Direct Cost: ¥273,000,000、Indirect Cost: ¥10,800,000)
Fiscal Year 2001: ¥46,800,000 (Direct Cost: ¥36,000,000、Indirect Cost: ¥10,800,000)
Fiscal Year 2000: ¥36,000,000 (Direct Cost: ¥36,000,000)
Fiscal Year 1999: ¥68,000,000 (Direct Cost: ¥68,000,000)
Fiscal Year 1998: ¥133,000,000 (Direct Cost: ¥133,000,000)
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| Keywords | Bioactivity / Total synthesis / Isolation of activities / Nerve affecting / Antibiotics / Practical synthesis / Chiral synthesis / Molecular design / 抗エイズ薬 / 抗痴〓薬 / 抗痴呆薬 |
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| Research Abstract |
1. The total synthesis and developments of 12 kinds of natural products possessing multiple bioactivities have been accomplished : for examples : (1) central nervous affecting and antifungal products ES242s ; (2) antifungal, cholesterol lowering and nerve growth factor affecting calbistrins; (3) antibacterial and antitumor pyralomicins; (4) one of big four antibiotics, tetracycline ; (5) antitumor and antibacterial quinolactacins ; and (6) insulin receptor affecting, antitumor and anti-HIV, asterriquinones. Remarkably, a new methodology have been developed by using ^<15>N-NMR studies for clarification of the structure - activity relationship. As a result, several medicinally useful compounds were found to show stronger activities than the mother natural products.
2. New sysnthetic methods have been delveloped. (1) synthesis of prenylphenols by convenient method combining three segments using palladium catalysts ; (2) direct preparation of aldehydes and ketones from the corresponding carboxylic acids ; (3) synthetic studies on natural products containing tetrahydro-pyrans and furans, and antitumor antibiotics, taxols and ustiloxins.
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