药学学报, 2017, 52(1): 120-125
引用本文:
杨雨, 左建, 李家明, 马晓东, 张艳春, 黄伟军. 苯丙烯酰胺类化合物的设计、合成及抗血小板聚集活性[J]. 药学学报, 2017, 52(1): 120-125.
YANG Yu, ZUO Jian, LI Jia-ming, MA Xiao-dong, ZHANG Yan-chun, HUANG Wei-jun. Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation[J]. Acta Pharmaceutica Sinica, 2017, 52(1): 120-125.

苯丙烯酰胺类化合物的设计、合成及抗血小板聚集活性
杨雨1,2, 左建1,2, 李家明1,2, 马晓东1,2, 张艳春1,2, 黄伟军1,2
1. 安徽中医药大学药学院, 安徽 合肥 230038;
2. 安徽省中医药科学院药物化学研究所, 安徽 合肥 230038
摘要:
依据拼合原理,设计并合成了20个具有苯丙烯酰胺类结构的化合物,其结构均经IR、1H NMR、13C NMR和MS确证。采用Bron比浊法测定了所有化合物对二磷酸腺苷(adenosine diphoshate,ADP)及花生四烯酸(arachidonic acid,AA)诱导的血小板聚集的抑制活性。初步药理结果显示,化合物6b、9b、9d9h对AA诱导的血小板聚集具有较好的抑制作用;化合物6b、6d、6j、9b9g对ADP诱导的血小板聚集具有较好的抑制作用。
关键词:    苯丙烯酰胺      合成      抗血小板聚集      血栓烷A2      钙离子拮抗剂     
Design, synthesis, and biological evaluation of phenylpropenamides compounds as anti-platelet aggregation
YANG Yu1,2, ZUO Jian1,2, LI Jia-ming1,2, MA Xiao-dong1,2, ZHANG Yan-chun1,2, HUANG Wei-jun1,2
1. College of Pharmacy, Anhui University of Chinese Medicine, Hefei 230038, China;
2. Deparment of Medicinal Chemistry, Anhui Academy of Chinese Medicine, Hefei 230038, China
Abstract:
Twenty phenylpropenamide analogs with structural novelty were designed and synthesized upon pharmacophore-combination strategy. The structures of target compounds were elucidated by IR, 1H NMR, 13C NMR and MS, and all the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by adenosine diphoshate (ADP) and (AA) arachidonic acid via Bron method. As a result, compounds 6b, 9b, 9d and 9h demonstrated potent inhibitory activity against platelet aggregation induced by AA. Meanwhile, compounds 6b, 6d, 6j, 9b and 9g exhibited significant suppression of platelet aggregation induced by ADP.
Key words:    phenylpropenamides    synthesis    anti-platelet aggregation    TXA2    Ca2+ inhibitor   
收稿日期: 2016-10-30
DOI: 10.16438/j.0513-4870.2016-1049
基金项目: 国家创新药物孵化基地项目(2012ZX09401066).
通讯作者: 李家明,Tel:86-551-68129147,Fax:86-551-65169222,E-mail:lijiaming2004@sina.com
Email: lijiaming2004@sina.com
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