Synthesis and preliminary evaluation of danshensu derivatives modified at hydroxyl group
- Author:
Qing-Bin CUI
1
Author Information
1. Institute of New Drug Research, Jinan University
- Publication Type:Journal Article
- Keywords:
Cardioprotection;
Chemical synthesis;
Danshensu derivatives
- From:
Journal of International Pharmaceutical Research
2013;40(6):795-800
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize Danshensu derivatives to study the role of hydroxyl group n Danshensu's bio-activity. Methods The phenolic and carboxyl groups of Danshensu were protected by benzyl, and then he hydroxyl group underwent reaction with different catalysts o get hydroxyl modified derivatives through ether and ester bonds, then benzyl groups were removed o get target derivatives. These derivatives were evaluated n H9c2 cells against tert-butyl hydroperoxide induced injury o illustrate the structure-activity relationship. Results Eleven derivatives were synthesized, and heir structures were confirmed by MS, NMR and elemental analysis. Biological results showed that neither ether nor ester derivatives showed better anti-oxidative effects than Danshensu. Conclusion The free hydroxyl group may be necessary for Danshensu's activity.
