Project/Area Number |
20790105
|
Research Category |
Grant-in-Aid for Young Scientists (B)
|
Allocation Type | Single-year Grants |
Research Field |
Drug development chemistry
|
Research Institution | Kobe Pharmaceutical University |
Principal Investigator |
OKITSU Takashi Kobe Pharmaceutical University, 薬学部, 助教 (50441209)
|
Project Period (FY) |
2008 – 2009
|
Project Status |
Completed (Fiscal Year 2009)
|
Budget Amount *help |
¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2009: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2008: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
|
Keywords | 医薬分子設計 / 核内受容体 / レチノイド / RXR / RAR / テルペノイド / メタボリック症候群 / 癌 / Stilleカップリング / Stileカップリング |
Research Abstract |
The ligand molecules of retinoid X receptors (RXRs) are candidates for therapeutic agents of metabolic syndrome such as dyslipidemia and type II diabete. The natural ligand of RXR is 9Z-retinoic acid so that I have developed an efficient synthesis of 9Z-rerinoic acid and its analogs. Among them, (-)-menthol congener had strong RXRα agonist activity. It is noteworthy that an analog having indole showed isotype selectivity (RXRα>γ). In the process of my project, I also discovered novel iodocyclizations leading to benzofurans and spiro compounds.
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