2017年9月
Structure-activity relations of rosmarinic acid derivatives for the amyloid beta aggregation inhibition and antioxidant properties
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- 巻
- 138
- 号
- 開始ページ
- 1066
- 終了ページ
- 1075
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.ejmech.2017.07.026
- 出版者・発行元
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
Amyloid-beta aggregation inhibitors are expected to be therapeutic or prophylactic agents for Alzheimer's disease. Rosmarinic acid, which is one of the main aggregation inhibitors derived from Lamiaceae, was employed as a lead compound and its 25 derivatives were synthesized. In this study, the structure activity relations of rosmarinic acid derivatives for the amyloid-beta aggregation inhibitory effect (MSHTS assay), antioxidant properties, and xanthine oxidase inhibition were evaluated. Among the tested compounds, compounds 16d and 19 were found to the most potent amyloid aggregation inhibitors. The SAR revealed that the necessity of the presence of the phenolic hydroxyl on one side of the molecule as well as the lipophilicity of the entire molecule. The importance of these structural properties was also supported by docking simulations. (C) 2017 Elsevier Masson SAS. All rights reserved.
- リンク情報
-
- DOI
- https://doi.org/10.1016/j.ejmech.2017.07.026
- PubMed
- https://www.ncbi.nlm.nih.gov/pubmed/28759879
- Web of Science
- https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:000411297000082&DestApp=WOS_CPL
- Scopus
- https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=85026353002&origin=inward
- Scopus Citedby
- https://www.scopus.com/inward/citedby.uri?partnerID=HzOxMe3b&scp=85026353002&origin=inward
- URL
- http://europepmc.org/abstract/med/28759879
- ID情報
-
- DOI : 10.1016/j.ejmech.2017.07.026
- ISSN : 0223-5234
- eISSN : 1768-3254
- ORCIDのPut Code : 48887465
- PubMed ID : 28759879
- SCOPUS ID : 85026353002
- Web of Science ID : WOS:000411297000082