Synthesis and anti-myocardial ischemia activities of novel Danshensu derivatives
10.3969/j.issn.1006-0111.2015.06.012
- VernacularTitle:新型丹参素衍生物的合成与抗心肌缺血活性研究
- Author:
Lin TIAN
1
;
Haixia GUO
;
Jie ZHANG
;
Yuqiang JIAO
;
Qiuye WU
;
Chuan ZHANG
Author Information
1. 福建中医药大学药学院
- Keywords:
Danshensu;
structure modification;
synthesis;
pharmacological activity
- From:
Journal of Pharmaceutical Practice
2015;(6):525-528,535
- CountryChina
- Language:Chinese
-
Abstract:
Objective To design and synthesize novel Danshensu derivatives in order to improve their stability and cardio-protective effect against myocardial ischemia .Methods Novel Danshensu derivatives were synthesized chiefly viaesterification , methoxy phenol hydroxyl protection ,nitration and amine solution reaction .All the target compounds were evaluated their bio-logical effects on anti-myocardial ischemia with H9c2 cells in vitro .Results 15 compounds were synthesized and further con-firmed by 1 H NMR and MS .Pharmacological studies showed that few synthetic derivatives at 5μmol/L performed a higher bi-ological effect than Danshensu .Conclusion Most derivatives didn't show the best activity at the chosen concentration gradient that a further pharmacological trial need to be done .