刘万冬,朱盼虎,李家明,王贤娜,童萍萍.化学通报,2019,82(3):275-279.
奥拉西坦衍生物的设计、合成及抗血小板聚集活性研究
Design, synthesis, and Anti-Platelet Aggregation Activities evaluation of oxiracetam derivatives
投稿时间:2018-09-06  修订日期:2018-11-08
DOI:
中文关键词:  奥拉西坦  吲哚布芬  抗血小板聚集  缺血性脑卒中
英文关键词:oxiracetam  indobufen anti-platelet  aggregation ischemic  stroke
基金项目:安徽省重大科技专项(15czz01077)
作者单位E-mail
刘万冬 安徽中医药大学药学院 合肥 wandongliu1115@163.com 
朱盼虎 安徽中医药大学药学院 合肥  
李家明* 安徽中医药大学药学院 合肥 lijiaming2017@sina.com 
王贤娜 安徽中医药大学药学院 合肥  
童萍萍 安徽中医药大学药学院 合肥  
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中文摘要:
      本文采用拼合策略,设计、合成了7个新型奥拉西坦衍生物。其中,化合物4a-f由奥拉西坦与苯丙烯酸片段拼合得到;4g则由奥拉西坦、吲哚布芬拼合得到。采用Bron比浊法测定目标化合物对花生四烯酸(arachidonic acid AA)及二磷酸腺苷(adenosine diphoshate ADP)诱导的血小板聚集的抑制活性。结果表明该系列化合物具有一定的抗血小板聚集活性,其中化合物4f的抗血小板聚集活性与阳性对照吲哚布芬相当。
英文摘要:
      Herein, seven novel oxiracetam derivatives were designed and synthesized upon employing pharmacophore-combination strategy. Among them, compounds 4a-f were attained via structurally combining oxiracetam with cinnamylic acid fragment, while compounds 4g were attained via combining oxiracetam with indobufen through ester functionality. All the target compounds were biologically evaluated for the inhibitory activities of platelet aggregation induced by arachidonic acid (AA) and adenosine diphoshate (ADP) via Bron method. The results of in vitro anti-platelet aggregation activities showed that the compounds had certain anti-platelet aggregation activity, and the anti-platelet aggregation activity of compound 4f was consistent with that of the positive control indobuprofen.
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