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奥拉西坦衍生物的设计、合成及抗血小板聚集活性研究

本站小编 Free考研考试/2021-12-27

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:oxiracetamindobufen anti-plateletaggregation ischemicstroke 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
摘要点击次数:1340 全文下载次数:0 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. 查看全文查看/发表评论下载PDF阅读器 相关附件:版权转让声明书 -->
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