| Project/Area Number |
23590140
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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 | Kinki University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
MINEMATSU Toshie 近畿大学, 薬学部, 助手 (60088151)
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| Project Period (FY) |
2011 – 2013
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | サラシノール / α-グルコシダーゼ阻害剤 / αーグルコシダーゼ阻害剤 / 3'-O-アルキル化 / サラシア / 構造活性相関 |
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| Research Abstract |
To develop more potent alpha-glucosidase inhibitors whose seed-compound is salacinol (1), a potent natural alpha-glucosidase inhibitor isolated from Salacia reticulata of Ayurvedic traditional medicine, several candidates with 3'-O-alkyl (CH3, C2H5, C13H27) or benzyl groups (CH2C6H5, CH2C6H4CH3, CH2C6H5Cl, CH2C6H4CF3, CH2C6H4NO2) instead of the 3'-O-sulfate anion in 1 were synthesized. These analogs showed equal or considerably higher inhibitory activity against rat small intestinal alpha-glucosidases than 1. Among the sulfonium salts designed, one with 3'-O-(ortho-nitrobenzyl) moiety was found to be the most potent, and ca. forty times as potent as 1, the compound being the strongest inhibitor among the sulfonium type inhibitors synthesized so far.
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