Design, synthesis, and neuroprotective and anti-platelet aggregation research of 3-n-butylphthalide derivatives
10.16438/j.0513-4870.2019-0969
- VernacularTitle:丁苯酞衍生物的设计、合成及神经细胞保护和抗血小板聚集活性研究
- Author:
Bin ZHANG
1
;
Wan-dong LIU
1
;
Jia-ming LI
1
;
Fan JIN
1
;
Shi-hu QIAN
1
Author Information
1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China
- Publication Type:Research Article
- Keywords:
3-n-butylphthalide derivative;
ischemic stroke;
neuroprotective effect;
anti-platelet aggregation
- From:
Acta Pharmaceutica Sinica
2020;55(3):478-483
- CountryChina
- Language:Chinese
-
Abstract:
Butylphthalide and ferulic acid exhibit excellent therapeutic effects in ischemic stroke. In this research, twelve 3-n-butylphthalide derivatives were designed by molecular hybridization strategy. The target compounds were obtained by nucleophilic substitution, reduction reaction, esterification reaction and elimination reaction, and the structure was confirmed by 1H NMR, 13C NMR and ESI-MS. All compounds were evaluated for neuroprotective activity against OGD/R-induced neurotoxicity in rat cortical neurons by MTT assay. The compounds with the best neuroprotective activity were biologically evaluated for their ability to inhibit platelet aggregation induced by arachidonic acid (AA) and adenosine diphosphate (ADP) via the Bron method．The results indicate that 7b exhibited potent neurocyte protective activity as well as prominent anti-platelet aggregation activity. Compound 7b has potential to be developed as a drug for ischemic stroke.
