Development and mechanistic study of novel anti-Alzheimer's disease drugs based on physiologically active fatty acid

基于生理活性脂肪酸的新型抗阿尔茨海默病药物的开发及作用机制研究

• 批准号: 20890266
• 负责人: SHIMIZU Tadashi
• 金额: $ 2.11万
• 依托单位: Hyogo University of Health Sciences
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Young Scientists (Start-up)
• 财政年份: 2008
• 资助国家: 日本
• 起止时间: 2008 至 2009
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-20890266/
• 关键词: 認知症治療剤; 生理活性脂肪酸; 光学分割; 光学活性誘導体; シクロプロパン; DCP-LA

We have already reported linoleic acid analogues without unstable cis-double bonds, called DCP-LA, which induced LTP-like long-lasting facilitation of hippocampal neurotransmission in both in vitro and in vivo systems. However, DCP-LA was four stereo-isomer mixtures, the determination of the most active isomer have been remained. In this reserch, we have developed synthetic route for the preparation of all of the four isomers of enantiomerically pure DCP-LA employing lipase-mediated resolution method, and found the most active stereoisomers.

我们已经报道了不含不稳定顺式双键的亚油酸类似物，称为DCP-LA，其在体外和体内系统中诱导LTP样持久促进海马神经传递。但是，DCP-LA是四种立体异构体的混合物，活性最强的异构体的测定方法一直存在争议。本研究采用脂肪酶介导的拆分方法，对DCP-LA的四种异构体进行了合成，并找到了活性最高的立体异构体。

项目成果

Improvement of monolithic solid material by utilization of spacer for identification of the target using affinity resins

• DOI: 10.1016/j.bmcl.2009.01.050
• 发表时间: 2009-03-01
• 期刊: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
• 影响因子: 2.7
• 作者: Iwaoka, Emiko;Mori, Tomoko;Tanaka, Akito
• 通讯作者: Tanaka, Akito

Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα(PKCα)

异苯并呋喃酮衍生物的不对称合成及其作为蛋白激酶Cα(PKCα)的独特特性

• 发表时间: 2009
• 期刊: Tetarahedron Letters 50
• 作者: G. Hirai;Y. Ogoshi;M. Ohkubo;Y. Tamura;T. Watanabe;T. Shimizu;M. Sodeoka;長環;Go Hirai
• 通讯作者: Go Hirai

Asymmetric synthesis of isobenzo furanone derivatives and their unique character as protein kinase Cα(PKCα).

异苯并呋喃酮衍生物的不对称合成及其作为蛋白激酶Cα(PKCα)的独特特性。

• 发表时间: 2009
• 期刊: Teterahedron Lett. 50
• 作者: G. Hirai;Y. Ogoshi;M. Ohkubo;Y. Tamura;T. Watanabe;T. Shimizu;M. Sodeoka
• 通讯作者: M. Sodeoka