2015 Fiscal Year Final Research Report
Design, synthesis and biological evaluation of pyripyropene A truncated analogs as ACAT2 selective inhibitor
| Project/Area Number |
25460152
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University |
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Principal Investigator |
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Keywords | 創薬化学 / 構造活性相関 / ACAT / 有機合成化学 |
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| Outline of Final Research Achievements |
Pyripyropene A, isolated from the culture broth of Aspergillus fumigatus FO-1289, is currently the only compound known to strongly and selectivity inhibit the acyl-CoA: cholesterol acyltransferase 2 (ACAT2) isozyme. To assist the development of new cholesterol-lowering or anti-atherosclerotic agents, we designed new A-ring truncated pyripyropene A analogs. We report here our successful synthesis of truncated analogs via a stereoselective intramolecular Michael cyclization method, and the construction of a 6-pyridyl-alfa-pyrone moiety.
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| Free Research Field |
創薬化学
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