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サラシノールをシードとする高活性スルホニウム塩型食後過血糖改善薬の合成と活性評価
https://kindai.repo.nii.ac.jp/records/13987
https://kindai.repo.nii.ac.jp/records/139873258edec-a570-454f-b015-fb8f4aa846ab
名前 / ファイル | ライセンス | アクション |
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KAKEN_23590140seika.pdf (308.4 kB)
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Item type | 研究報告書 / Research Paper(1) | |||||
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公開日 | 2014-09-29 | |||||
タイトル | ||||||
タイトル | サラシノールをシードとする高活性スルホニウム塩型食後過血糖改善薬の合成と活性評価 | |||||
その他(別言語等)のタイトル | ||||||
その他のタイトル | Synthesis and evaluation of sulfonium-type alpha-glucosidase inhibitors based on the structure of salacinol | |||||
著者 |
田辺, 元三
× 田辺, 元三× 峯松, 敏江 |
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言語 | ||||||
言語 | jpn | |||||
キーワード | ||||||
主題 | サラシノール, α-グルコシダーゼ阻害剤 | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_18ws | |||||
資源タイプ | research report | |||||
著者(英) | ||||||
en | ||||||
TANABE, Genzo | ||||||
著者(英) | ||||||
en | ||||||
MINEMATSU, Toshie | ||||||
著者 所属 | ||||||
近畿大学薬学部; 准教授 | ||||||
著者 所属 | ||||||
近畿大学薬学部; 助手 | ||||||
著者 役割 | ||||||
研究代表者 | ||||||
著者 役割 | ||||||
研究分担者 | ||||||
著者 外部リンク | ||||||
関連名称 | http://kaken.nii.ac.jp/d/r/40217104.ja.html | |||||
著者 外部リンク | ||||||
関連名称 | http://kaken.nii.ac.jp/d/r/60088151.ja.html | |||||
版 | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
出版者 名前 | ||||||
出版者 | 近畿大学 | |||||
書誌情報 |
科学研究費助成事業研究成果報告書 (2013. ) p. 1-6, 発行日 2013-01-01 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 研究成果の概要(和文): Salacinol (1)は, アーユルベーダ医学における糖尿病の特効薬物(Salacia reticulata)から単離された強いα-グルコシダーゼ阻害作用を示す化合物である. 今回, 1の側鎖部3'位疎水性化置換基を種々検討し, その誘導体の合成および活性評価を行った結果, メチル基を除くアルキル基およびベンジル基をもつ化合物に, 著しい活性の向上が認められ, 中でも, 3'-0-(o-ニトロベンジル)体が1の約40倍強力な活性を示し, 糖尿病治療薬, acarbose, vogliboseを凌駕する活性を示すことを明らかにした. 研究成果の概要(英文): 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'-0-alkyl (CH3, C2H5, C13H27) or benzyl groups (CH2C6H5, CH2C6H4CH3, CH2C6H5C1, CH2C6H4CF3, CH2C6H4NO2) instead of the 3'-0-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'-0-(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. | |||||
内容記述 | ||||||
内容記述タイプ | Other | |||||
内容記述 | 研究種目:基盤研究(C); 研究期間:2011~2013; 課題番号:23590140 ; 研究分野:医歯薬学; 科研費の分科・細目:創薬化学 | |||||
資源タイプ | ||||||
内容記述タイプ | Other | |||||
内容記述 | Research Paper | |||||
フォーマット | ||||||
内容記述タイプ | Other | |||||
内容記述 | application/pdf |